Home Immunology & Inflammation IL Receptor 조절자 Dexamethasone

연구용

Dexamethasone Glucocorticoid Receptor 작용제

제품 번호S1322

Dexamethasone은 글루코코르티코이드 스테로이드 약물 계열의 강력한 합성 구성원이며, 항염증 및 면역억제 효과를 가지는 인터루킨 수용체 조절자입니다. Dexamethasone은 autophagy 및 mitophagy를 유도합니다. Dexamethasone은 COVID-19로 입원한 환자에게 시험되었으며 중증 환자에게 유익한 것으로 밝혀졌습니다.
Dexamethasone IL Receptor 조절자 Chemical Structure

화학 구조

분자량: 392.46

바로가기

품질 관리

배치: 순도: 99.68%
99.68

세포 배양, 처리 및 작업 농도

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
human monocytes Function assay 5 μM 20 h Antiinflammatory activity in human monocytes assessed as inhibition of LPS-induced COX2 expression at 5 uM after 20 hrs using rabbit polyclonal antibody IgG by SDS-PAGE analysis 21843935
rat polymorphonuclear leukocytes Function assay 20 mins Antiinflammatory activity in rat polymorphonuclear leukocytes assessed as inhibition of LPS-stimulated nitric oxide production after 20 mins by Griess method, IC50=2.3 nM 22506620
mouse thymocytes Function assay 1 μM 24 h Induction of apoptosis in mouse thymocytes assessed as internucleosomal DNA fragmentation at 1 uM after 24 hrs by agarose gel electrophoresis 24794748
T-cell Function assay Inhibitory concentration against T cell proliferation using concanavalin A stimulated mice spleen cells, IC50 = 0.005 μM. 11229767
PBMC Function assay Inhibitory concentration against TNF-alpha production from human peripheral blood mononuclear cells stimulated by LPS, IC50 = 0.01 μM. 11229767
PBMC Function assay Inhibitory concentration against growth of LPS stimulated human peripheral blood mononuclear cells, IC50 = 0.04 μM. 11229767
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as effect on TNFalpha formation pretreated 1 hr before LPS challenge measured after 24 hrs, IC50 = 0.7 μM. 11908984
N9 Function assay Inhibitory activity against TNF-alpha release in N9 cells in the supernatant, IC50 = 0.074 μM. 12361395
RAW 264.7 Function assay Inhibitory activity against TNF-alpha release in RAW 264.7 cells in the supernatant, IC50 = 0.42 μM. 12361395
A549 Function assay 10 uM Antagonist activity for Glucocorticoid receptor in MMTV transactivation assay in human A549 lung epithelial cells at 10 uM, IC50 = 10 μM. 15999989
A549 Function assay Activity at glucocorticoid receptor in human A549 cells assessed as effect on GRE promoter response by luciferase reporter assay, EC50 = 0.001 μM. 16643060
A549 Function assay Agonist activity at GR assessed as MMTV-mediated transactivation of renilla luciferase gene in human A549 cells relative to Dexamethasone, EC50 = 0.005012 μM. 16821781
A549 Function assay Agonist activity at GR assessed as NF-kappaB-mediated transrepression of secreted placental alkaline phosphatase gene in human A549 cells, IC50 = 0.001175 μM. 16821781
HFF Function assay Induction of aromatase activity in HFF cells assessed as production of beta estradiol by aromatase assay, EC50 = 0.0019 μM. 17181172
HeLa Function assay Activation of MMTV in HeLa cells measured by luciferase activity, EC50 = 0.017 μM. 17181172
HFF Function assay Inhibition of IL1-stimulated IL6 production in HFF cells, IC50 = 0.00051 μM. 17181172
RAW 264.7 Function assay 24 hrs Inhibition of interferon gamma-stimulated NO production in RAW 264.7 cells after 24 hrs, IC50 = 0.02 μM. 17367124
RAW264.7 Function assay 2 hrs Inhibition of COX2 expression in LPS-stimulated mouse RAW264.7 cells after 2 hrs by Western blot analysis 17407277
RAW264.7 Function assay 2 hrs Inhibition of mPGES1 expression in LPS-stimulated mouse RAW264.7 cells after 2 hrs by Western blot analysis 17407277
A549 Function assay Agonist activity at glucocorticoid receptor in human A549 cells by MMTV transactivation assay, EC50 = 0.00537 μM. 17616395
A549 Function assay Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay, IC50 = 0.001 μM. 17616395
A549 Function assay Antagonist activity at glucocorticoid receptor in human A549 cells transfected with MMTV luciferase reporter gene assessed as inhibition of dexamethasone-induced activation, IC50 = 1 μM. 17616395
HFF Antiinflammatory assay Antiinflammatory activity assessed as inhibition of IL1 stimulated IL6 production in HFF cells by transrepression assay, EC50 = 0.0005 μM. 17692519
HFF Antiinflammatory assay Antiinflammatory activity assessed as upregulation of aromatase in HFF cells by transactivation assay, EC50 = 0.002 μM. 17692519
CV1 Function assay Agonist activity at human GR expressed in CV1 cells by GRE activation assay, EC50 = 0.0002 μM. 17705362
NHDFneo Function assay Activity at human GR expressed in NHDFneo cells assessed as inhibition of IL-6 production, IC50 = 0.0014 μM. 17705362
RPMI8226 Antiproliferative assay 4 days Antiproliferative activity against human RPMI8226 cells after 4 days, IC50 = 0.0065 μM. 17705362
J774A.1 Function assay Inhibition of LPS-induced TNFalpha production in mouse J774A.1 cells, IC50 = 0.048 μM. 17892941
CV1 Function assay Activity at human glucocorticoid receptor expressed in CV1 cells assessed as repression of TNF and IL-1-beta-induced E-selectin gene expression by luciferase reporter gene assay, ED50 = 0.0001 μM. 18032610
A549 Function assay Agonist activity at glucocorticoid receptor in human A549 cells by MMTV transactivation assay, EC50 = 0.005012 μM. 18038970
A549 Function assay Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay, IC50 = 0.001175 μM. 18038970
COS7 Function assay 1 uM Agonist activity at glucocorticoid receptor Q570A mutant in COS7 cells at 1 uM by NF-kappaB-luciferase reporter gene assay 18038970
HeLa Cytotoxicity assay Cytotoxicity against human HeLa cells assessed as inhibition of DNA replication by imaging analysis 18066055
HeLa Function assay Inhibition of mitosis in human HeLa cells by imaging analysis 18066055
R1 Function assay 10 uM 24 hrs Inhibition of glucocorticoid receptor-glucocorticoid complex transfected in rat R1 cells assessed as down-regulation of TPA-responsive element proinflammatory gene expression at 10 uM after 24 hrs by beta-galactosidase assay, IC50 = 0.005 μM. 18412397
THP1 Antiinflammatory assay Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL6 by ELISA, IC50 = 0.007 μM. 18625560
THP1 Antiinflammatory assay Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha by ELISA, IC50 = 0.05 μM. 18625560
RAW264.7 Function assay 10 uM Inhibition of LPS-stimulated COX2 expression in mouse RAW264.7 cells at 10 uM by Western blot 18790649
RAW264.7 Function assay Inhibition of LPS-stimulated microsomal prostaglandin E synthase 1 expression at 10 uM in mouse RAW264.7 cells by Western blot 18790649
A549 Function assay Transrepression activity at GR in IL-1-beta-stimulated human A549 cells assessed as inhibition of NF-kappaB-dependent E-selectin transcription by luciferase reporter gene assay, EC50 = 0.0011 μM. 19321341
A549 Function assay Transrepression activity at GR in PMA-stimulated human A549 cells assessed as inhibition of AP1 response element-induced luciferase reporter gene activity, EC50 = 0.0025 μM. 19321341
NP1 Function assay Agonist activity at GR ligand binding domain expressed in human NP1 cells assessed as glucocorticoid response element transactivation by GAL4 luciferase reporter gene assay, EC50 = 0.0042 μM. 19321341
TH2 Function assay 48 hrs Inhibition of pro-inflammatory cytokine IL5 production in ovalbumin-stimulated BALB/c mouse TH2 cells after 48 hrs by sandwich-ELISA, IC50 = 0.005 μM. 19323483
TH2 Function assay 48 hrs Inhibition of pro-inflammatory cytokine IL13 production in ovalbumin-stimulated BALB/c mouse TH2 cells after 48 hrs by sandwich-ELISA, IC50 = 0.005 μM. 19323483
MDA-kb2 Function assay Agonist activity at androgen receptor in human MDA-kb2 cells assessed as stimulation of luciferase activity by luciferase reporter gene assay, EC150 = 0.194 μM. 19592245
MDA-kb2 Function assay Agonist activity at glucocorticoid receptor in human MDA-kb2 cells assessed as stimulation of luciferase activity by luciferase reporter gene assay, EC150 = 0.194 μM. 19592245
A549 Function assay Agonist activity at GR in human A549 cells by NF-kappaB transrepression assay, IC50 = 0.001 μM. 19592247
COS7 Function assay Agonist activity at glucocorticoid receptor ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay, EC50 = 0.0072 μM. 19863083
A549 Function assay 6 hrs Transrepression activity at glucocorticoid receptor expressed in human A549 cells assessed as inhibition of IL-1-beta-induced NF-kappaB dependent E-selection promoter activation after 6 hrs by luciferase reporter gene based ELAM assay, EC50 = 0.0011 μM. 20047280
A549 Function assay 6 hrs Transrepression activity at glucocorticoid receptor expressed in human A549 cells assessed as inhibition of PMA-induced AP1 activity after 6 hrs by luciferase reporter gene assay, EC50 = 0.0025 μM. 20047280
HeLa Function assay Transactivation of GAL-4 tagged glucocorticoid receptor ligand binding domain expressed in human HeLa cells assessed as NP1 activation by luciferase reporter gene assay, EC50 = 0.0045 μM. 20047280
NIH-3T3 Function assay 0.01 mg/kg 1 hr Plasma concentration in mouse bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 0.01 mg/kg, po after 1 hr, Cp = 0.044 μM. 20469868
NIH-3T3 Function assay 0.1 mg/kg 1 hr Plasma concentration in mouse bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 0.1 mg/kg, po after 1 hr, Cp = 0.236 μM. 20469868
NIH-3T3 Function assay 1 mg/kg 1 hr Plasma concentration in mouse bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 1 mg/kg, po after 1 hr, Cp = 1.8 μM. 20469868
NIH-3T3 Function assay 10 mg/kg 1 hr Plasma concentration in mouse bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 10 mg/kg, po after 1 hr, Cp = 17.7 μM. 20469868
NIH-3T3 Function assay 0.01 mg/kg 1 hr Fraction unbound in mouse plasma bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 0.01 mg/kg, po after 1 hr, Fu = 0.00203 μM. 20469868
NIH-3T3 Function assay 0.1 mg/kg 1 hr Fraction unbound in mouse plasma bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 0.1 mg/kg, po after 1 hr, Fu = 0.0116 μM. 20469868
NIH-3T3 Function assay 1 mg/kg 1 hr Fraction unbound in mouse plasma bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 1 mg/kg, po after 1 hr, Fu = 0.087 μM. 20469868
NIH-3T3 Function assay 10 mg/kg 1 hr Fraction unbound in mouse plasma bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 10 mg/kg, po after 1 hr, Fu = 5.123 μM. 20469868
HeLa Function assay Transactivation activity at glucocorticoid receptor in human HeLa cells assessed as induction of MMTV promoter activity by luciferase reporter gene assay, EC50 = 0.007943 μM. 20727743
HeLa Function assay Transrepression activity at glucocorticoid receptor-mediated antiinflammatory activity in human HeLa cells assessed as inhibition of TPA-induced collagenase promoter activity by luciferase reporter gene assay, IC50 = 0.001585 μM. 20727743
THP1 Function assay Transrepression activity at glucocorticoid receptor-mediated antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL-8 production, IC50 = 0.002512 μM. 20727743
Sf9 Function assay Binding affinity to human recombinant glucocorticoid receptor expressed in baculovirus infected Sf9 cells, IC50 = 0.01259 μM. 20727743
insect cells Function assay Binding affinity to glucocorticoid receptor expressed in baculovirus-infected insect cells using tetramethylrhodamine labeled Dexamethasone by fluorescence polarization microplate assay, IC50 = 0.0034 μM. 20735001
insect cells Function assay Binding affinity to mineralocorticoid receptor expressed in baculovirus-infected insect cells using tetramethylrhodamine labeled Dexamethasone by fluorescence polarization microplate assay, IC50 = 0.033 μM. 20735001
U2OS Function assay 18 hrs Agonist activity at glucocorticoid receptor-LBD in human U2OS cells transfected with Gal4-DBD assessed as increase of transactivation activity after 18 hrs by luciferase reporter gene assay, EC50 = 15.8489 μM. 20812681
U2OS Function assay 18 hrs Antagonist activity at glucocorticoid receptor-LBD in human U2OS cells transfected with Gal4-DBD assessed as inhibition of transactivation activity after 18 hrs by luciferase reporter gene assay, IC50 = 0.0005082 μM. 20812681
HepG2 Function assay 24 hrs Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis, EC50 = 2.6 μM. 20966043
A549 Function assay Transrepression activity of glucocorticoid receptor in human A549 cells assessed as inhibition of IL1beta-stimulated NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay, EC50 = 0.0011 μM. 21073190
A549 Function assay Transrepression activity of glucocorticoid receptor in human A549 cells expressing AP-1 assessed as inhibition of PMA-induced AP-1 activity by luciferase reporter gene assay, EC50 = 0.0025 μM. 21073190
NP-1 Hela Function assay Transactivation activity of glucocorticoid receptor ligand binding domain expressed in human NP-1 Hela cells co-expressing GAL4 DNA binding domain by luciferase reporter gene assay, EC50 = 0.0042 μM. 21073190
13D3/Huh7 Function assay 24 hrs Transactivation activity at glucocorticoid receptor in human 13D3/Huh7 cells assessed as induction of tyrosine aminotransferase activity after 24 hrs, EC50 = 0.005 μM. 21073190
A549 Function assay Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay, IC50 = 0.001 μM. 21257309
A549 Function assay Agonist activity at GR in human A549 cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activity, IC50 = 0.003981 μM. 21257309
RAW264.7 Antiinflammatory assay 18 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production treated 2 hrs before LPS challenge measured after 18 hrs by griess reaction, IC50 = 0.86 μM. 21288727
HMC1 Function assay 1 hr Immunomodulatory activity in human HMC1 cells assessed as inhibition of phorbol 12-myristate 13-acetate/A23187-stimulated IL1-beta secretion treated 1 hr prior to 30 mins phorbol 12-myristate 13-acetate/A23187 challenge by Western blotting analysis 21302967
RAW264.7 Antiinflammatory assay 10 uM 24 hrs Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as nitrite level at 10 uM after 24 hrs by Griess method, Activity = 1.54 μM. 21353543
RAW264.7 Antiinflammatory assay 18 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha secretion after 18 hrs, IC50 = 0.01 μM. 21353543
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess method, IC50 = 0.8 μM. 21353543
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFN-gamma induced NO production after 24 hrs by Griess reaction, IC50 = 0.02 μM. 21361338
RAW264.7 Function assay 20 mins Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells pre-incubated for 20 mins before LPS challenge measured 18 hrs post LPS challenge by Griess method 21775152
RAW264.7 Function assay 30 mins Inhibition of LPS-induced TNFalpha production in mouse RAW264.7 cells pre-incubated for 30 mins before LPS challenge measured 6 hrs post LPS challenge by ELISA 21775152
HeLa Function assay Agonist activity at glucocorticoid receptor in human HeLa cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activity, EC50 = 0.017 μM. 21963986
insect cells Function assay Displacement of tetramethylrhodamine-labeled Dexamethasone from human recombinant glucocorticoid receptor expressed in baculovirus infected insect cells by fluorescence polarization assay, IC50 = 0.003 μM. 21963986
insect cells Function assay Displacement of tetramethylrhodamine-labeled Dexamethasone from human recombinant mineralocorticoid receptor expressed in baculovirus infected insect cells by fluorescence polarization assay, IC50 = 0.033 μM. 21963986
RAW264.7 Antiinflammatory assay 2 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated nitric oxide production pretreated for 2 hrs before LPS challenge measured after 18 hrs by Griess method, IC50 = 0.47 μM. 22372956
RAW264.7 Antiinflammatory assay 2 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production pretreated for 2 hrs before LPS challenge measured after 18 hrs by Griess method, IC50 = 0.98 μM. 22537362
A549 Antiinflammatory assay 1 uM 30 mins Antiinflammatory activity in human A549 cells assessed as inhibition of IL-1beta-induced mPGES1 expression at 1 uM treated 30 mins prior to IL-1beta challenge measured after 48 hrs by Western blot analysis relative to control 22795900
H13 Function assay 3 hrs Inhibition of glucocorticoid receptor in human H13 cells assessed as inhibition of glucocorticoid-induced cell proliferation after 3 hrs by [3H]-thymidine incorporation assay, EC50 = 0.0097 μM. 23199485
293 MSR Function assay 60 mins Displacement of [3H]-dexamethasone human glucocorticoid receptor alpha expressed in 293 MSR cells after 60 mins by scintillation counting, EC50 = 0.0125 μM. 23199485
IOBA-NHC Function assay 40 uM 24 hrs Inhibition of NF-kappaB p65-mediated IL-6 release in HSV1 KOS infected human IOBA-NHC cells at 40 uM after 24 hrs by ELISA 23219855
IOBA-NHC Function assay 40 uM 24 hrs Inhibition of NF-kappaB p65-mediated TNFalpha release in HSV1 KOS infected human IOBA-NHC cells at 40 uM after 24 hrs by ELISA 23219855
IOBA-NHC Function assay 40 uM 24 hrs Inhibition of NF-kappaB p65-mediated IL-8 release in HSV1 KOS infected human IOBA-NHC cells at 40 uM after 24 hrs by ELISA 23219855
HCLE Function assay 40 uM 24 hrs Inhibition of NF-kappaB p65-mediated IL-8 release in HSV1 KOS infected human HCLE cells at 40 uM after 24 hrs by ELISA 23219855
HCT116 Function assay 20 to 40 uM 24 hrs Agonist activity at glucocorticoid receptor (unknown origin) expressed in human HCT116 cells co-expressing GRE at 20 to 40 uM after 24 hrs by luciferase reporter gene assay 23276449
RAW264.7 Antiinflammatory assay 2 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production incubated for 2 hrs prior to LPS-challenge measured after 24 hrs by Griess method, IC50 = 1.43 μM. 23373965
HeLaS3 Function assay 2 hrs Displacement of [3H]Dexamethasone from glucocorticoid receptor in human HeLaS3 cells after 2 hrs, IC50 = 0.0041 μM. 23403082
HeLaS3 Function assay 2 hrs Displacement of [3H]Dexamethasone from glucocorticoid receptor in human HeLaS3 cells after 2 hrs, Ki = 0.0022 μM. 23403082
A549 Function assay Transrepression activity at glucocorticoid receptor in human A549 cells assessed as inhibition of IL1beta-stimulated NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay, EC50 = 0.0011 μM. 23916594
A549 Function assay Transrepression activity at glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-stimulated AP1 response element by luciferase reporter gene assay, EC50 = 0.0025 μM. 23916594
Hela Function assay Transactivation activity at glucocorticoid receptor ligand binding domain (unknown origin) expressed in human Hela cells co-expressing GAL4 DNA binding domain assessed as NP-1-stimulated GRE activation by luciferase reporter gene assay, EC50 = 0.0045 μM. 23916594
A549 Function assay Agonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of IL-1beta-induced NF-kappaB dependent E-selectin activation by luciferase reporter gene assay, EC50 = 0.0011 μM. 23953070
A549 Function assay Agonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-induced AP-1 activation by luciferase reporter gene assay, EC50 = 0.0025 μM. 23953070
HeLa Function assay Transactivation of glucocorticoid receptor ligand binding domain (unknown origin) transfected in human HeLa cells assessed as activation of NP-1 by GAL4 luciferase reporter gene assay, EC50 = 0.0045 μM. 23953070
A549 Function assay Transrepression of glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-induced AP-1 activity by luciferase reporter gene assay, EC50 = 0.0025 μM. 24011644
HeLa Function assay Transactivation of GR-LBD expressed in human HeLa cells co-expressing GAL4-DBD by luciferase reporter gene assay, EC50 = 0.0042 μM. 24011644
HEK293 Function assay Displacement of [3H]-aldosterone from human mineralocorticoid receptor expressed in HEK293 cells, Ki = 0.00036 μM. 24446728
HEK293 Function assay Displacement of [3H]-dexamethasone from human glucocorticoid receptor expressed in HEK293 cells, Ki = 0.00069 μM. 24446728
HEK293 Function assay Displacement of [3H]-methyltrienolone from human progesterone receptor expressed in HEK293 cells, Ki = 0.561 μM. 24446728
HEK293 Function assay Displacement of [3H]-methyltrienolone from human androgen receptor expressed in HEK293 cells, Ki = 1.41 μM. 24446728
HeLa Function assay Transactivation of glucocorticoid receptor in human HeLa cells harboring MMTV promoter by luciferase reporter gene assay, EC50 = 0.017 μM. 24656565
A549 Function assay Agonist activity at glucocorticoid receptor in human A549 cells assessed as E-selectin transrepression by luciferase reporter gene assay, EC50 = 0.0011 μM. 24980053
A549 Function assay Agonist activity at glucocorticoid receptor in human A549 cells assessed as AP-1 transrepression by luciferase reporter gene assay, EC50 = 0.0025 μM. 24980053
HeLa Function assay Agonist activity at glucocorticoid receptor in human HeLa cells assessed as NP-1 transactivation by luciferase reporter gene assay, EC50 = 0.0045 μM. 24980053
B16F10 Antitumor assay 20 mg/kg 24 days Antitumor activity against mouse B16F10 cells xenografted in C57BL/6 mouse assessed as inhibition tumor growth at 20 mg/kg, ip measured after 24 days of tumor inoculation 24992071
B16F10 Antitumor assay 20 mg/kg 24 days Antitumor activity against mouse B16F10 cells xenografted in C57BL/6 mouse assessed as apoptotic regions at 20 mg/kg, ip measured after 24 days of tumor inoculation by TUNEL assay 24992071
B16F10 Apoptosis assay 10 uM 48 hrs Induction of apoptosis in mouse B16F10 cells assessed as increase in ratio of BAX/Bcl2 expression at 10 uM after 48 hrs by Western blot analysis relative to untreated control 24992071
B16F10 Antitumor assay 20 mg/kg 24 days Antitumor activity against mouse B16F10 cells xenografted in C57BL/6 mouse assessed as apoptotic regions at 20 mg/kg, ip measured after 24 days of tumor inoculation by VE-cadherin 24992071
CUTLL1 Growth inhibition assay 48 hrs Growth inhibition of human CUTLL1 cells with high GR expression levels after 48 hrs by alamar blue assay 25050160
HEK293 Function assay Agonist activity at human GCR expressed in HEK293 cells by luciferase reporter gene assay, EC50 = 0.0013 μM. 25305688
RAW264.7 Function assay 24 hrs Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay relative to vehicle-treated control, IC50 = 0.8 μM. 25499882
HFF Function assay Agonist activity at GR in HFF cells assessed as suppression of IL-1-induced IL-6 production, IC50 = 0.001 μM. 25516791
RAW264.7 Antiinflammatory assay 1 mM 30 mins Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction of LPS-induced TNF mRNA expression cells at 1 mM treated 30 mins before LPS challenge measured after 3 hrs by qRT-PCR analysis 25667960
SW1353 Function assay 24 hrs Transrepression activity at glucocorticoid receptor in human SW1353 cells assessed as repression of IL-1-induced MMP-13 production after 24 hrs by ELISA, IC50 = 0.0018 μM. 25706100
RAW264.7 Function assay 6 hrs Inhibition of TNFalpha production in mouse RAW264.7 cells incubated for 6 hrs by sandwich immunoassay, IC50 = 0.04 μM. 25824662
J774A.1 Function assay 6 hrs Inhibition of TNFalpha production in mouse J774A.1 cells incubated for 6 hrs by sandwich immunoassay, IC50 = 0.4 μM. 25824662
RAW264.7 Function assay 12 hrs Inhibition of IL-1beta production in mouse RAW264.7 cells incubated for 12 hrs by sandwich immunoassay, IC50 = 4.7 μM. 25824662
J774A.1 Function assay 12 hrs Inhibition of IL-1beta production in mouse J774A.1 cells incubated for 12 hrs by sandwich immunoassay, IC50 = 22 μM. 25824662
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay, IC50 = 0.63 μM. 26087384
BV2 Antiinflammatory assay 24 hrs Antiinflammatory activity in C57BL6/J mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay, IC50 = 0.025 μM. 26110443
RAW264.7 Function assay 24 hrs Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay, IC50 = 0.8 μM. 26305406
J774 Antiinflammatory assay 10 uM 24 hrs Antiinflammatory activity against mouse J774 cells assessed as inhibition of LPS-induced iNOS expression at 10 uM after 24 hrs by Western blot analysis 26915998
IM9 Function assay Displacement of [3H]dexamethasone from glucocorticoid receptor in human IM9 cells, IC50 = 0.0038 μM. 26988801
C57BL/6 Antiinflammatory assay 10 mg/kg 1 hr Antiinflammatory activity in C57BL/6 mouse assessed as inhibition of zymosan-induced mononuclear cells migration in articular cavity at 10 mg/kg, ip administered 1 hr prior to zymosan challenge measured at 6 to 24 hrs 27227459
C57BL/6 Antiinflammatory assay 10 mg/kg 1 hr Antiinflammatory activity in C57BL/6 mouse assessed as inhibition of zymosan-induced infiltration of inflammatory cells into synovial tissue at 10 mg/kg, ip administered 1 hr prior to zymosan challenge measured at 6 to 24 hrs by hematoxylin and eosin stai 27227459
J774A.1 Antiinflammatory assay 1 uM 1 hr Antiinflammatory activity in mouse J774A.1 cells assessed as inhibition of zymosan and IFNgamma-induced IL6 production in cell-free supernatant at 1 uM preincubated for 1 hr followed by zymosan and IFNgamma addition measured after 24 hrs by sandwich ELISA 27227459
J774A.1 Antiinflammatory assay 1 uM 1 hr Antiinflammatory activity in mouse J774A.1 cells assessed as inhibition of zymosan and IFNgamma-induced COX2 expression at 1 uM preincubated for 1 hr followed by zymosan and IFNgamma addition measured after 24 hrs by Western blot analysis 27227459
J774A.1 Antiinflammatory assay 1 uM 1 hr Antiinflammatory activity in mouse J774A.1 cells assessed as inhibition of zymosan and IFNgamma-induced nitric oxide production at 1 uM preincubated for 1 hr followed by zymosan and IFNgamma addition measured after 24 hrs by colorimetric Griess test 27227459
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs in presence of LPS by Griess assay, IC50 = 0.63 μM. 27825545
IM9 Function assay Displacement of [3H]dexamethasone from GR receptor in human IM9 cells, IC50 = 0.0038 μM. 27876250
HeLa Function assay Transrepression activity at glucocorticoid receptorin human HeLa cells assessed as inhibition of TPA-induced collagenase promoter activity by luciferase reporter gene assay, IC50 = 0.001585 μM. 28043796
THP1 Function assay Transrepression activity at glucocorticoid receptor in human THP1 cells assessed as receptor-mediated anti-inflammatory activity by measuring inhibition of LPS-induced IL-8 production, IC50 = 0.002512 μM. 28043796
HeLa Function assay Transactivation activity at glucocorticoid receptor in human HeLa cells assessed as induction of MMTV promoter activity by luciferase reporter gene assay, IC50 = 0.007943 μM. 28043796
Sf9 Function assay Binding affinity to recombinant human glucocorticoid receptor expressed in baculovirus infected sf9 cells, IC50 = 0.01259 μM. 28043796
RAW264.7 Antiinflammatory assay 30 mins Antiinflammatory activity in mouse RAW264.7 cells assessed as reduction in LPS-induced NO production pretreated for 30 mins followed by LPS stimulation for 24 hrs by Griess assay, IC50 = 7 μM. 28499733
RAW264.7 Function assay 24 hrs Inhibition of LPS-induced NO production in mouse RAW264.7 cells after 24 hrs by Griess assay, IC50 = 2.5 μM. 28598633
Mino Antiproliferative assay 100 uM 48 hrs Antiproliferative activity against human Mino cells at 100 uM preincubated for 48 hrs followed by thymidine addition measure after 16 hrs by Thymidine incorporation assay 28858511
RAW264.7 Antiinflammatory assay Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production by griess assay, IC50 = 0.8 μM. 29272126
RAW264.7 Function assay 10 uM 1 hr Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in COX2 mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR analysi 29389121
RAW264.7 Function assay 10 uM 1 hr Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in iNOS mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR analysi 29389121
RAW264.7 Function assay 10 uM 1 hr Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in TNFalpha mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR ana 29389121
RAW264.7 Function assay 10 uM 1 hr Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in IL-1beta mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR ana 29389121
RAW264.7 Function assay 10 uM 1 hr Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in IL-6 mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR analysi 29389121
RAW264.7 Function assay 10 uM 1 hr Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in NO production at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 24 hrs by Grie 29389121
RAW264.7 Function assay 10 uM 1 hr Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in IL-1beta production at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 24 hrs b 29389121
RAW264.7 Function assay 10 uM 1 hr Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in IL-6 production at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 24 hrs by EL 29389121
RAW264.7 Function assay 10 uM 1 hr Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in TNFalpha production at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 3 hrs by 29389121
RAW264.7 Function assay 10 uM 1 hr Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in iNOS protein level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 24 hrs by 29389121
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BV2 Antiinflammatory assay Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production, IC50 = 9.5 μM. 29482940
RAW264.7 Function assay 24 hrs Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay, IC50 = 10.7 μM. 29518326
HeLa Function assay 0.4 uM 24 hrs Transrepression of GCR in human HeLa cells assessed as suppression of DEX-induced GILZ mRNA expression at 0.4 uM after 24 hrs by Taqman-based real-time PCR analysis 29670697
RAW264.7 Antiinflammatory assay Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production, IC50 = 8.3 μM. 29741372
HEK 293T Function assay Agonist activity at GAL4 DNA-binding domain fused GR (unknown origin) ligand binding domain expressed in UAS-bla HEK 293T cells assessed as beta-lactamase transcriptional activation by FRET-based GeneBLAzer assay, IC50 = 0.00235 μM. 30144697
RAW264.7 Antiinflammatory assay 20 uM 6 hrs Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 production at 20 uM pretreated for 6 hrs followed by LPS stimulation measured after 24 hrs by ELISA 30215255
RAW264.7 Antiinflammatory assay 20 uM 6 hrs Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-1beta production at 20 uM pretreated for 6 hrs followed by LPS stimulation measured after 24 hrs by ELISA 30215255
RAW264.7 Antiinflammatory assay 20 uM 6 hrs Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrite production at 20 uM pretreated for 6 hrs followed by LPS stimulation measured after 24 hrs by ELISA 30215255
RAW264.7 Antiinflammatory assay 20 uM 6 hrs Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production at 20 uM pretreated for 6 hrs followed by LPS stimulation measured after 24 hrs by ELISA 30215255
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량 392.46 화학식

C22H29FO5

 보관 (수령일로부터) 2 years 4°C, in dark and seal
CAS 번호 50-02-2 SDF 다운로드 원액 보관

동의어 NSC 34521, Hexadecadrol, Prednisolone F,MK-125 Smiles CC1CC2C3CCC4=CC(=O)C=CC4(C3(C(CC2(C1(C(=O)CO)O)C)O)F)C

용해도

In vitro
배치:

DMSO : 78 mg/mL (198.74 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 11 mg/mL

Water : Insoluble

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

mg/kg g μL

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘

Targets/IC50/Ki
interleukin receptor
(Cell-free assay)
시험관 내(In vitro)

Dexamethasone은 불멸화된 쥐 뇌 내피세포주(GPNT)에서 주로 수크로스, 플루오레세인 및 20 KDa까지의 덱스트란에 대한 단일층 경유 세포간 투과성을 감소시킵니다. 이 화합물은 배양된 쥐 뇌 내피세포에서 필라멘트형 액틴과 세포골격 관련 단백질 코르탁틴이 세포-세포 접촉 부위에 고농도로 집중되고, 세포질 내에는 F-액틴 스트레스 섬유가 거의 보이지 않게 하는데, 이는 이 화학물질에 의해 유도된 더 분화된 장벽 표현형과 일치하는 관찰입니다. 이 치료법은 세포 분화에 관여하는 혈청 유도성 헬릭스-루프-헬릭스 전사 억제제인 Id-1 단백질 수준을 강력하게 자극하는 것으로 나타났으며, 이 효과는 Con8 유방 상피 종양 세포에서 ZO-1의 세포 주변부 재조직과 관련이 있는 것으로 나타났습니다. 이는 처리되지 않은 GPNT 단일층에서 사이토카인 유도 MMP-9 발현 증가 및 ZO-1 발현 변화를 방지합니다.

이 화합물은 폐포 상피세포에서 AP-1(c-Jun)을 포함하는 메커니즘을 통해 감마-GCS-중쇄 서브유닛 전사를 하향 조절함으로써 기저 및 TNF-알파 자극 GSH 수준을 모두 고갈시킵니다. 이는 폐포 상피세포(A549)에서 GSSG의 변화 없이 기저 및 자극 GSH 수준(TNF-α 처리)을 모두 감소시킵니다.

생체 내(In vivo)

Dexamethasone은 임신한 암양에게 근육주사로 투여되며, 다음과 같은 결과를 초래합니다: (1) 혈압은 변하지 않습니다; (2) 태아에서 이전에 보고된 바와 같이, 엔도텔린-1(ET)에 대한 민감도가 증가합니다; (3) 아세틸콜린 유도 이완이 증가합니다; (4) L-NAME에 의해 억제될 수 있는 ET에 대한 혈관 확장 반응이 없어집니다; (5) 내피세포 비의존성 혈관 확장에는 변화가 없습니다; 그리고 (6) 식염수 처리 대조군과 비교할 때 eNOS RNA 및 단백질 수준에는 변화가 없습니다.

참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/16166452/
  • [5] https://pubmed.ncbi.nlm.nih.gov/17440100/
  • [6] https://pubmed.ncbi.nlm.nih.gov/28263313/
  • [7] https://pubmed.ncbi.nlm.nih.gov/35544603/

적용 분야

방법 바이오마커 이미지 PMID
Western blot Bcl-2 / Bcl-xl / Mcl-1 / Survivin / IAP1 Cyclin D1 / Cyclin E / COX-2 / MMP-9 Bax / p21 p-JNK / JNK / p-p38 / p38 / p-ERK / ERK
S1322-WB1
28696369

임상시험 정보

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호 모집 조건 스폰서/협력자 시작일 단계
NCT06351644 Not yet recruiting
Relapsed and/or Refractory Multiple Myeloma
Adriana Rossi|Icahn School of Medicine at Mount Sinai
 June 3 2024 Phase 1|Phase 2
NCT06367855 Not yet recruiting
Spinal Stenosis Lumbar|Disc Degeneration|Disc Disease|Fusion of Spine|Surgery
Potsawat Surabotsopon|Thammasat University Hospital
 May 1 2024 Phase 4
NCT06367725 Recruiting
Acute Lymphoblastic Leukemia
University of Aarhus
 April 11 2024 --

기술 지원

취급 설명서

Tel: +1-832-582-8158 Ext:3

다른 문의사항이 있으시면 메시지를 남겨주세요.

이름을 입력해주세요.
이메일을 입력해주세요. 유효한 이메일 주소를 입력해주세요.
저희에게 무엇이든 작성해주세요.

자주 묻는 질문

질문 1:
I'm looking for it to use in cell culture. Would it be better to use the S1322, the sodium phosphate S4028, or the acetate S3124?

답변:
S1322 is the free base form of this compound, S4028 is the sodium phosphate form and S3124 is the acetate salt. All of them have similar biological activity in tissue culture, however, their suitabilities vary in different solvents. As free base, S1322 has high solubility in DMSO (79mg/ml), poor solubility in water (<1mg/ml), and moderate solubility in ethanol (6mg/ml). As sodium phosphate salt, S4028 has high solubility in water (103mg/ml) but is insoluble in DMSO and ethanol (<1mg/ml). The solubility of S3124 is 87mg/ml in DMSO, <1mg/ml in water, and 20mg/ml in ethanol. Selection can be made based on the customer's experimental setup.