연구용
제품 번호: S2256
화학 구조
| 세포주 | 분석 유형 | 농도 | 배양 시간 | 제형 | 활성 설명 | PMID |
|---|---|---|---|---|---|---|
| COS1 cells | Function assay | Agonistic activity was determined in COS1 cells transfected with GAL 4-PPAR gamma receptor, EC50=0.021 μM | ||||
| CV-1 cells | Function assay | Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay, EC50=0.043 μM | ||||
| COS-1 cells | Function assay | In vitro transactivation of human peroxisome proliferator activated receptor gamma measured in PPAR-GAL4 chimeric COS-1 cells, EC50=0.02 μM | ||||
| CV-1 cells | Function assay | Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection assay in CV-1 cells, EC50=0.08913 μM | ||||
| CV-1 cells | Function assay | In vitro transcriptional activation of Peroxisome proliferator activated receptor gamma (PPAR) expressed in CV-1 cells, EC50=0.06 μM | ||||
| COS-1 cells | Function assay | In vitro agonist activity tested for transactivation in human PPAR gamma-Gal4 chimeric COS-1 cells, EC50=0.02 μM | ||||
| CV-1 cells | Function assay | In vitro evaluation against RXR-alpha/PPAR-gamma in CV-1 cells by cotransfection assay was determined, EC50=0.325 μM | ||||
| HepG2 cells | Function assay | Effective concentration against human PPARgamma expressed in HepG2 cells, EC50=0.039 μM | ||||
| Huh7 cells | Function assay | Functional activity at human PPAR gamma in Huh7 cells by transactivation assay, EC50=0.22 μM | ||||
| Huh7 cells | Function assay | Effect on PPAR gamma transactivation activity in Huh7 cells, EC50=0.22 μM | ||||
| U2OS cells | Function assay | Effect on PPARgamma transactivation activity in U2OS cells, EC50=0.03 μM | ||||
| CV1 cells | Function assay | Transactivation of PPARgamma in CV1 cells, EC50=0.076 μM | ||||
| human keratinocytes | Proliferation assay | Antiproliferative activity against human keratinocytes, EC50=8 μM | ||||
| HT29 cell | Proliferation assay | Antiproliferative activity against human HT29 cell line, EC50=45 μM | ||||
| NIH3T3 cells | Function assay | Activity at human PPAR gamma transfected in NIH3T3 cells by luciferase activity assay, EC50=0.32 μM | ||||
| CV1 cells | Function assay | Transactivation of human PPARgamma in CV1 cells by luciferase reporter gene assay, EC50=0.308 μM | ||||
| Huh7 cells | Function assay | Activity at human PPAR gamma in Huh7 cells by transactivation assay, EC50=0.22 μM | ||||
| HepG2 cells | Function assay | Agonist activity at human PPAR gamma in a HepG2 cells by PPAR-GAL4 transactivation assay, EC50=0.158 μM | ||||
| HepG2 cells | Function assay | Agonist activity at human PPAR gamma in HepG2 cells by PPAR-GAL4 transactivation assay, EC50=0.158μM | ||||
| CV1 cells | Function assay | Activity at human PPARgamma in CV1 cells, EC50=0.308 μM | ||||
| HEK293 cells | Function assay | Activity at human adipose tissue PPAR gamma expressed in HEK293 cells by PPAR-GAL4 transactivation assay, EC50=0.31 μM | ||||
| rat L6 cells | Function assay | Effect on fatty acid oxidation in rat L6 cells, EC50=5 μM | ||||
| HepG2 cells | Function assay | Agonist activity at human PPARgamma in HepG2 cells by PPAR-GAL4 transactivation assay, EC50=0.082 μM | ||||
| CV1 cells | Function assay | Agonist activity at human PPARalpha in CV1 cells by GAL4 transactivation assay after 24 hrs, EC50=3.46 μM | ||||
| CV1 cells | Function assay | Agonist activity at human PPARgamma in CV1 cells by GAL4 transactivation assay after 24 hrs, EC50=0.03 μM | ||||
| CV1 cells | Function assay | Agonist activity at human PPARgamma expressed in CV1 cells by receptor transactivation assay, EC50=0.308 μM | ||||
| CV1 cells | Function assay | Agonist activity at PPARgamma in CV1 cells by transactivation assay, EC50=0.308 μM | ||||
| HEK293 cells | Function assay | Agonist activity at PPARgamma receptor expressed in HEK293 cells by GAL4 transactivation assay, EC50=0.035 μM | ||||
| NIH3T3 cells | Function assay | Agonist activity at human PPARgamma expressed in NIH3T3 cells by GAL4 transactivation assay, EC50=0.32 μM | ||||
| HEK293 cells | Function assay | Agonist activity at PPARgamma expressed in HEK293 cells by GAL4 transactivation assay, EC50=0.19 μM | ||||
| HEK293 cells | Function assay | Agonist activity at PPARgamma expressed in HEK293 cells assessed as aP2 gene induction, EC50=0.12 μM | ||||
| HEK293 cells | Function assay | Agonist activity at PPARgamma in HEK293 cells by GAL4 transactivation assay, EC50=0.045 μM | ||||
| HepG2 cells | Function assay | Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with Gal4 by luciferase reporter gene assay, EC50=0.039 μM | ||||
| RAW264.7 cells | Function assay | Suppression of LPS/IFN-gamma-stimulated NO production in mouse RAW264.7 cells, EC50=17.5 μM | ||||
| BL21 cells | Function assay | Displacement of radio labeled 2(S)-(2-benzoyl-phenylamino)-3-{4-[1,1-ditritio-2-(5-methyl-2-phenyl-oxazol-4-yl)-ethoxy]-phenyl}-propionic acid from GST-fused human PPARgamma expressed in Escherichia coli BL21 cells by scintillation proximity assay, EC50=0.45 μM | ||||
| BHK21 cells | Function assay | Agonist activity at human PPARgamma expressed in BHK21 cells assessed as SEAP activity by luciferase reporter transactivation assay, EC50=0.45 μM | ||||
| HepG2/C3A cells | Function assay | Activation of human PPARgamma ligand binding domain-mediated transcriptional activity in human HepG2/C3A cells co-transfected with fused Gal4-LBD by cotransfection assay, EC50=0.0038 μM | ||||
| HepG2 cells | Function assay | Agonist activity at PPARgamma expressed in human HepG2 cells assessed as induction of receptor transactivation by reporter gene assay relative to control, EC50=0.05 μM | ||||
| COS1 cells | Function assay | Agonist activity at human recombinant PPARgamma expressed in COS1 cells co-expressing GAL4 assessed as transcriptional activity after 48 hrs by luciferase reporter gene assay, EC50=0.02 μM | ||||
| HepG2 cells | Function assay | Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay, EC50=0.223 μM | ||||
| CV1 cells | Function assay | Agonist activity at human PPARgamma ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay, EC50=0.033 μM | ||||
| CV1 cells | Function assay | Agonist activity at human PPARalpha ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay, EC50=3.46 μM | ||||
| U2OS cells | Function assay | Agonist activity at human PPARgamma in U2OS cells by transactivation assay, EC50=0.02 μM | ||||
| Hep G2 cells | Function assay | Agonist activity at human PPARgamma ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay, EC50=0.04 μM | ||||
| HeLa cells | Function assay | Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay, EC50=0.015 μM | ||||
| COS1 cells | Function assay | Agonist activity at human PPARgamma receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay, EC50=0.02 μM | ||||
| U2OS cells | Function assay | Agonist activity at human PPARgamma expressed in U2OS cells by luciferase transactivation assay, EC50=0.05 μM | ||||
| HepG2 cells | Function assay | Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay, EC50=0.039 μM | ||||
| HepG2 cells | Function assay | Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay, EC50=0.223 μM | ||||
| COS7 cells | Function assay | Agonist activity at human recombinant PPARgamma2 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay, EC50=0.1 μM | ||||
| COS7 cells | Function assay | Agonist activity at human recombinant PPARgamma1 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay, EC50=0.03 μM | ||||
| HEK cells | Function assay | Agonist activity at human GAL4-tagged PPARalpha chimeric receptor expressed in HEK cells by transactivation assay, EC50=10.58 μM | ||||
| HEK cells | Function assay | Agonist activity at human GAL4-tagged PPARgamma chimeric receptor expressed in HEK cells by transactivation assay, EC50=0.035 μM | ||||
| 3T3L1 cells | Function assay | 7 days | Induction of adipogenesis in mouse 3T3L1 cells assessed as increase in lipid accumulation after 7 days by Oil red O staining | |||
| CHO-K1 cells | Function assay | Partial agonist activity at human PPARgamma-LBD expressed in CHO-K1 cells co-transfected with GAL4 assessed as luciferase activity by transactivation assay, EC50=0.1 μM | ||||
| HEK293T cells | Function assay | 1 μM | 24 hrs | Partial agonist activity at human PPARgamma-LBD expressed in HEK293T cells assessed as induction of receptor transactivation at 1 uM after 24 hrs by luciferase reporter gene assay | ||
| CV1 cells | Function assay | Transactivation of Gal4-fused human PPARgamma DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay, EC50=0.1 μM | ||||
| HEK293 cells | Function assay | 16 to 20 hrs | Transactivation of Gal4-fused human PPARgamma expressed in HEK293 cells after 16 to 20 hrs by luciferase reporter gene assay, EC50=0.043 μM | |||
| HepG2 cells | Function assay | 10 umol/L | 24 hrs | Increase in glucose consumption in human HepG2 cells at 10 umol/L after 24 hrs relative to control | ||
| 3T3L1 cell | Function assay | 1 uM | Induction of mouse 3T3L1 cell differentiation assessed as increase in accumulation of intracellular lipid droplet at 1 uM by Oil red O staining | |||
| CV1 cells | Function assay | 40 h | Agonist activity at human PPARgamma-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay, EC50=0.1 μM | |||
| HepG2 cells | Function assay | Agonist activity at PPARgamma receptor expressed in human HepG2 cells by PPRE-luciferase reporter gene assay, EC50=0.01 μM | ||||
| HepG2 cells | Function assay | Transactivation of human PPARgamma expressed in human HepG2 cells co-transfected with PPRE3-TK-Luc by luciferase reporter gene assay, EC50=0.05 μM | ||||
| COS7 cells | Function assay | Modulation of human PPARgamma-LBD expressed in african green monkey COS7 cells co-transfected with Gal4 assessed as activation of transactivation activity by luciferase assay, EC50=0.043 μM | ||||
| COS-1 cells | Function assay | 24 hrs | Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis, EC50=0.048 μM | |||
| COS1 cells | Function assay | 24 hrs | Transactivation of human full length PPARgamma expressed in COS1 cells co-transfected with RXRalpha after 24 hrs by luciferase reporter gene assay, EC50=0.12 μM | |||
| MG-63 cells | Function assay | Agonist activity at human PPARgamma expressed in MG-63 cells by reporter gene-based transactivation assay, EC50=0.011 μM | ||||
| COS1 cells | Function assay | Binding affinity to human wild type PPARgamma LBD expressed in COS1 cells co-expressing GAL4 by scintillation proximity assay | ||||
| MG-63 cells | Function assay | 24 hrs | Modulation of full-length human pSG5-fused PPARgamma expressed in MG-63 cells co-expressing pGV-P2-PPRE after 24 hrs by luciferase reporter gene based transactivation assay, EC50=0.011 μM | |||
| Ac2F cells | Function assay | 0.1 to 10 μM | 6 hrs | Agonist activity at PPARgamma in rat Ac2F cells assessed as luciferase activity at 0.1 to 10 uM after 6 hrs by reporter gene assay | ||
| 293H DA cells | Function assay | 16 h | Agonist activity at PPARgamma LBD in human 293H DA cells after 16 hrs by TR-FRET activation reporter assay, EC50=0.0024 μM | |||
| 3T3L1 cells | Function assay | 10 uM | Increase in adiponectin mRNA levels in TNFalpha-induced mouse 3T3L1 cells pretreated at 10 uM before TNF-alpha challenge relative to control | |||
| HepG2 cells | Function assay | 10 uM | 24 h | Reduction of glucose consumption in insulin-resistant human HepG2 cells at 10 uM after 24 hrs by glucose oxidase method in presence of 22.2 mM of glucose | ||
| HepG2 cells | Function assay | 10 uM | 24 h | Reduction of glucose consumption in insulin-resistant human HepG2 cells at 10 uM after 24 hrs by glucose oxidase method in presence of 0.1 uM of insulin | ||
| THP1 cells | Function assay | 100 uM | 3 hrs | Transactivation of PPARgamma in human THP1 cells assessed as decrease in LPS-induced MCP1 mRNA expression at 100 uM preincubated for 3 hrs prior to LPS challenge measured after 18 hrs by RT-PCR analysis relative to untreated control | ||
| THP1 cells | Function assay | 100 uM | 3 hrs | Transactivation of PPARgamma in human THP1 cells assessed as decrease in LPS-induced IL6 mRNA expression at 100 uM preincubated for 3 hrs prior to LPS challenge measured after 18 hrs by RT-PCR analysis relative to untreated control | ||
| HepG2 cells | Function assay | Transactivation of GAL4-fused PPARgamma ligand binding domain transfected in human HepG2 cells by luciferase reporter gene assay, EC50=0.1 μM | ||||
| HepG2 cells | Function assay | 20 h | Agonist activity at human GAL4-fused PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene transactivation assay, EC50=0.02 μM | |||
| BL21 DE3 cells | Function assay | Displacement of [3H]rosiglitazone from N-terminal His-tagged human PPARgamma ligand binding domain expressed in Escherichia coli BL21 DE3 cells by scintillation proximity assay, Ki=0.074 μM | ||||
| human L02 cells | Function assay | Agonist activity at PPARgamma-LBD expressed in human L02 cells co-expressing pGL3-SV40-GAL4 after 24 hrs by luciferase reporter gene based transactivation assay, EC50=0.9 μM | ||||
| HepG2 cells | Function assay | 20 h | Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene assay, EC50=0.039 μM | |||
| HEK293 cells | Function assay | 10 μM | Transactivation of PPARgamma (unknown origin) expressed in HEK293 cells co-transfected with AP2-PPRE at 10 uM by luciferase reporter gene assay | |||
| HEK293 cells | Function assay | Agonist at human PPARgamma LBD expressed in human HEK293 cells cotransfected with GAL4-Luc assessed as transcriptional activation by luciferase reporter gene assay, EC50=0.004 μM | ||||
| HEK293 cells | Function assay | 24 h | Transactivation of GAL4 DBD-fused human PPARgamma-LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay, EC50=0.1 μM | |||
| HEK293 cells | Function assay | 48 hrs | Agonist activity at human PPARgamma expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay, EC50=43.71 μM | |||
| HepG2 cells | Function assay | Agonist activity at GAL4-fused PPARgamma (unknown origin) expressed in human HepG2 cells by transactivation assay, EC50=0.01 μM | ||||
| HepG2 cells | Function assay | Agonist activity at GAL4-fused PPARgamma M463A mutant (unknown origin) expressed in human HepG2 cells by transactivation assay, EC50=0.002 μM | ||||
| L6 cells | Function assay | 24 hrs | Induction of glucose uptake in rat L6 cells pulsed with C14-deoxy glucose after 24 hrs in presence of insulin, EC50=4.49 μM | |||
| L6 cells | Function assay | 16 hrs | Increase in 2-[3H]-deoxyglucose uptake in rat L6 cells after 16 hrs by scintillation counting analysis, EC50=4.8 μM | |||
| DU145 cells | Cytotoxicity assay | 48 hrs | Cytotoxicity against human DU145 cells assessed as growth inhibition after 48 hrs by MTT assay, EC50=16 μM | |||
| PC3 cells | Cytotoxicity assay | 48 hrs | Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay, EC50=20.3 μM | |||
| MDA-MB-231 cells | Growth inhibition assay | 24 hrs | Growth inhibition of human MDA-MB-231 cells after 24 hrs by MTT assay, EC50=5.23 μM | |||
| HEK293 cells | Function assay | Agonist activity at human PPARgamma expressed in HEK293 cells by luciferase reporter gene assay, EC50=0.01 μM | ||||
| HepG2 cells | Function assay | 20 hrs | Transactivation of PPAR transfected in human HepG2 cells after 20 hrs by PPAR-luciferase assay, EC50=1.6 μM | |||
| HEK293 cells | Function assay | 24 hrs | Transactivation of PPARgamma (unknown origin) expressed in HEK293 cells incubated for 24 hrs by luciferase reporter gene assay | |||
| HepG2 cells | Function assay | Agonist activity at human GAL4-PPARgamma ligand binding domain expressed in human HepG2 cells by luciferase reporter gene assay, EC50=0.039 μM | ||||
| HEK293 cells | Function assay | 24 hrs | Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay, EC50=0.03 μM | |||
| HepG2 cells | Function assay | 20 hrs | Agonist activity at GAL4-DNA binding domain fused human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation incubated for 20 hrs by luciferase reporter gene assay, EC50=0.04 μM | |||
| HepaR cells | Function assay | 1 day | Agonist activity at PPARgamma in human HepaR cells assessed as increase in HMGCS2 gene expression at 1 uM incubated for 1 day by quantitative PCR method relative to untreated control | |||
| HepaR cells | Function assay | 1 uM | 1 day | Agonist activity at PPARgamma in human HepaR cells assessed as increase in ANGPTL4 gene expression at 1 uM incubated for 1 day by quantitative PCR method relative to untreated control | ||
| HepaR cells | Function assay | 1 uM | 1 day | Agonist activity at PPARgamma in human HepaR cells assessed as increase in FABP1 gene expression at 1 uM incubated for 1 day by quantitative PCR method relative to untreated control | ||
| HEK293 cells | Function assay | 10 μM | 24 hrs | Transactivation of PPAR-gamma (unknown origin) expressed in HEK293 cells at 10 uM after 24 hrs by luciferase reporter gene assay | ||
| C2C12 cells | Function assay | 30 μM | 2 h | Induction of 2-deoxy-[3H]-glucose uptake in mouse C2C12 cells at 30 uM after 2 hrs by liquid scintillation counting analysis | ||
| MCF7 cells | Function assay | 16 h | Agonist activity at human PPARgamma transfected in human MCF7 cells after 16 hrs by luciferase reporter gene assay, EC50=0.087 μM | |||
| HEK293 cells | Function assay | 10 μM | 24 h | Agonist activity at PPARgamma (unknown origin) expressed in HEK293 cells assessed as receptor transactivation at 10 uM incubated for 24 hrs by luciferase reporter gene assay | ||
| 클릭하여 더 많은 세포주 실험 데이터 보기 | ||||||
| 분자량 | 176.17 | 화학식 | C10H8O3 |
보관 (수령일로부터) | |
|---|---|---|---|---|---|
| CAS 번호 | 90-33-5 | SDF 다운로드 | 원액 보관 |
|
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| 동의어 | N/A | Smiles | CC1=CC(=O)OC2=C1C=CC(=C2)O | ||
|
In vitro |
DMSO
: 35 mg/mL
(198.67 mM)
Ethanol : 35 mg/mL Water : Insoluble |
|
In vivo |
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1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)
2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)
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.
(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)
| NCT 번호 | 모집 | 조건 | 스폰서/협력자 | 시작일 | 단계 |
|---|---|---|---|---|---|
| NCT05295680 | Recruiting | Primary Sclerosing Cholangitis |
Aparna Goel|Stanford University |
May 10 2023 | Phase 2 |