Home Proteases HIV Protease 억제제 Nelfinavir Mesylate

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Nelfinavir Mesylate HIV Protease 억제제

제품 번호S4282

Nelfinavir Mesylate는 Ki가 2 nM인 강력한 HIV Protease 억제제입니다.
Nelfinavir Mesylate HIV Protease 억제제 Chemical Structure

화학 구조

분자량: 663.89

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품질 관리

배치: 순도: 99.51%
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세포 배양, 처리 및 작업 농도

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
HeLa Function assay TP_TRANSPORTER: inhibition of TEA uptake (TEA: 10 uM) in OCT1-expressing HeLa cells, IC50=21.8μM. 10681378
Caco-2 Function assay TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical) (Daunorubicin: 5 uM) in Caco-2 cells, IC50=1.4μM. 10820137
MT-4 Antiviral assay Anti-HIV-1 activity against Wild type virus in MT-4 cells, ED50=0.02μM. 11543677
MT-4 Antiviral assay Anti-HIV-1 activity against mutant HIV-1 in MT-4 cells (mutation selected with compound 1), ED50=0.07μM. 11543677
MT-4 Antiviral assay Anti-HIV-1 activity against mutant HIV-1 in MT-4 cells (mutation selected with ritonavir), ED50=0.11μM. 11543677
MT-4 Antiviral assay Anti-HIV-1 activity against mutant HIV-1 in MT-4 cells (mutation selected with saquinavir), ED50=0.12μM. 11543677
MT-4 Antiviral assay Anti-HIV-1 activity against mutant HIV-1 in MT-4 cells (mutation selected with nelfinavir), ED50=2.44μM. 11543677
LLC-PK1 Function assay Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay, IC50=2.3μM. 12699389
LLC-PK1 Function assay TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells, IC50=2.3μM. 12699389
LLC-PK1 Function assay Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay, IC50=3.4μM. 12699389
LLC-PK1 Function assay TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells, IC50=3.4μM. 12699389
HEK Function assay TP_TRANSPORTER: increase in mitoxantrone intracellular accumulation in BCRP-expressing HEK cells, IC50=12.5μM. 15007102
CEM-SS Antiviral assay 6 days Antiviral activity against HIV1 3B infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect after 6 days by MTS assay, ED50=0.03μM. 15217281
HOG.R5 Antiviral assay 4 days Antiviral activity against HIV1 3B infected in human HOG.R5 cells after 4 days, IC50=0.09μM. 15217281
MT-4 Function assay Effective dose of compound required to inhibit replication of human immunodeficiency virus type 1 in MT-4 cells, ED50=0.02μM. 15537350
MT4 Antiviral assay Antiviral activity against HIV1 HXB2 in MT4 cells, IC50=0.32μM. 16458505
MT4 Antiviral assay Antiviral activity against HIV1 EP13 in MT4 cells, IC50=0.45μM. 16458505
PHA-PBMC Antiviral assay Antiviral activity against HIV1 BA-L isolate in human PHA-PBMC cells, IC50=0.007μM. 16913714
MT2 Antiviral assay Antiviral activity against HIV1 LAI isolate in human MT2 cells, IC50=0.01μM. 16913714
PHA-PBMC Antiviral assay Antiviral activity against HIV1 LAI isolate in human PHA-PBMC cells, IC50=0.014μM. 16913714
MT2 Antiviral assay Antiviral activity against HIV2 EHO isolate in human MT2 cells, IC50=0.02μM. 16913714
PHA-PBMC Antiviral assay Antiviral activity against multi drug-resistant HIV1 ET variant in human PHA-PBMC cells, IC50=0.032μM. 16913714
PHA-PBMC Antiviral assay Antiviral activity against multi drug-resistant HIV1 G variant in human PHA-PBMC cells, IC50=0.17μM. 16913714
PHA-PBMC Antiviral assay Antiviral activity against multi drug-resistant HIV1 C variant in human PHA-PBMC cells, IC50=0.31μM. 16913714
MT2 Antiviral assay Antiviral activity against HIV2 EHO in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.03μM. 17371811
MT2 Antiviral assay Antiviral activity against HIV1 LAI in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.032μM. 17371811
MT4 Antiviral assay Antiviral activity against HIV1 NL4-3 in MT4 cells by MTT assay, EC50=0.033μM. 17371811
MT4 Antiviral assay Antiviral activity against HIV1 GRL98065p20 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.08μM. 17371811
MT4 Antiviral assay Antiviral activity against ritonavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.21μM. 17371811
MT4 Antiviral assay Antiviral activity against amprenavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.22μM. 17371811
MT2 Antiviral assay Antiviral activity against HIV2 ROD in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.24μM. 17371811
MT4 Antiviral assay Antiviral activity against atazanavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.27μM. 17371811
MT4 Antiviral assay Antiviral activity against HIV1 GRL98065p30 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.27μM. 17371811
MT4 Antiviral assay Antiviral activity against HIV1 GRL98065p40 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.34μM. 17371811
MT4 Antiviral assay Antiviral activity against idinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.47μM. 17371811
MT4 Antiviral assay Antiviral activity against saquinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.48μM. 17371811
MT4 Antiviral assay Antiviral activity against lopinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.49μM. 17371811
MT2 Cytotoxicity assay Cytotoxicity against human MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay, CC50=8.1μM. 17371811
MT4 Antiviral assay Antiviral activity against HIV1 3B in MT4 cells by MTT assay, EC50=0.016μM. 17537628
MT4 Cytotoxicity assay Cytotoxicity against MT4 cells by MTT assay, LC50=11μM. 17537628
MT4 Antiviral assay 5 days Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay, EC50=0.018μM. 17576848
MT4 Antiviral assay 5 days Antiviral activity against HIV2 MS infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay, EC50=0.048μM. 17576848
CEM Antiviral assay 7 days Antiviral activity against HIV2 ROD with protease G17N/V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay, EC50=0.1μM. 17576848
CEM Antiviral assay 7 days Antiviral activity against HIV2 ROD with protease V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay, EC50=0.177μM. 17576848
CEM Antiviral assay 7 days Antiviral activity against HIV2 ROD with protease G17N mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay, EC50=0.199μM. 17576848
CEM Antiviral assay 7 days Antiviral activity against wild type HIV2 ROD infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay, EC50=0.281μM. 17576848
HEK293 Antiviral assay 48 hrs Antiviral activity against wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay, EC50=0.0058μM. 17638694
MT4 Antiviral assay 6 days Antiviral activity against wild type HIV1 NL4-3 infected in MT4 cells after 6 days by MTT assay, EC50=0.029μM. 17638694
MT4 Cytotoxicity assay 6 days Cytotoxicity against human MT4 cells after 6 days by MTT assay, CC50=8μM. 17638694
HEK293 Function assay 0.12 uM Inhibition of HIV1 NL4-3 proteins incorporation into virions transfected in HEK293 cells assessed as unprocessed gp160 Env protein at 0.12 uM by Western blot 17646410
HEK293 Function assay 0.12 uM Inhibition of HIV1 NL4-3 proteins incorporation into virions transfected in HEK293 cells assessed as aberrant Env protein at 0.12 uM by Western blot 17646410
MDCK2 Inhibition of human Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells, IC50=19.9μM. 17664327
MDR1 Function assay 20 uM Decrease in P-glycoprotein-mediated tenofovir disoproxil fumarate efflux in MDCK2 expressing human MDR1 cells at 20 uM 17664327
CEM-SS Antiviral assay 5 days Antiviral activity against HIV1 LAI infected in human CEM-SS cells assessed as reverse transcriptase activity after 5 days by MTT assay, IC50=0.002μM. 17950955
MOLT-4/3B Antiviral assay 4 days Antiviral activity against HIV1 3B infected in MOLT-4/3B cells assessed as inhibition of mature virus release measured after 4 days of infection by RT assay, EC50=0.029μM. 18316521
MT4 Antiviral assay Antiviral activity against HIV1 3B in human MT4 cells assessed as inhibition of viral-induced cytopathic effect by MTT method, EC50=0.016μM. 18426195
MT4 Cytotoxicity assay Cytotoxicity against human MT4 cells by MTT assay, CC50=11μM. 18426195
MT4 Antiretroviral assay Antiretroviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.023μM. 18541726
MT4 Antiretroviral assay Antiretroviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.028μM. 18541726
MT4 Antiviral assay Antiviral activity against Reverse transcriptase inhibitor-resistant Human immunodeficiency virus 1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.029μM. 18541726
MT4 Antiviral assay Antiviral activity against non nucleoside reverse transcriptase inhibitor-resistant Human immunodeficiency virus 1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.035μM. 18541726
MT4 Antiretroviral assay Antiretroviral activity against Human immunodeficiency virus 2 EHO infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.049μM. 18541726
MT4 Antiretroviral assay Antiretroviral activity against Human immunodeficiency virus 2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.05μM. 18541726
MT4 Antiretroviral assay Antiretroviral activity against Simian immunodeficiency virus MAC 251 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.05μM. 18541726
MT4 Antiviral assay Antiviral activity against Protease inhibitor-resistant Human immunodeficiency virus 1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.17μM. 18541726
MT4 Antiviral assay 5 uM Antiviral activity against HIV1 NL4-3 harboring L10F/L33F/M46I/I47V/Q58E/V82I/I84V/I85V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of GRL-02031 by E, EC50=0.011μM. 18955518
MT4 Antiviral assay Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of p24 gag protein production by ELISA, EC50=0.018μM. 18955518
MT2 Antiviral assay 7 days Antiviral activity against HIV1 LAI infected in human MT2 cells after 7 days by MTT assay, EC50=0.023μM. 18955518
MT4 Antiviral assay 5 uM Antiviral activity against HIV1 NL4-3 harboring L10F/V32I/M46I/I54M//A71V/I84V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of amprenavir by ELISA, EC50=0.17μM. 18955518
MT4 Antiviral assay 1 uM Antiviral activity against HIV1 NL4-3 harboring L23I/K43I/M46I/I50L/G51A/A71V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 1 uM of atazanavir by ELISA, EC50=0.21μM. 18955518
MT4 Antiviral assay 5 uM Antiviral activity against HIV1 NL4-3 harboring M46I/V82F/I84V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of ritonavir by ELISA, EC50=0.24μM. 18955518
MT4 Antiviral assay 5 uM Antiviral activity against HIV1 NL4-3 harboring L10I/G48V/I54V/L90M amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of saquinavir by ELISA, EC50=0.32μM. 18955518
MT4 Antiviral assay 1 uM Antiviral activity against HIV1 NL4-3 harboring L10F/M46I/I54V/V82A amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 1 uM of Lopinavir by ELISA, EC50=0.51μM. 18955518
MT4 Antiviral assay 5 uM Antiviral activity against HIV1 NL4-3 harboring L10F/L24I/M46I/L63P/A71V/G73S/V82T amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of indinavir by ELISA, EC50=0.65μM. 18955518
HeLa Antiviral assay 72 hrs Antiviral activity against HIV1 harboring capsid I201V mutant protein infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay, EC50=0.013μM. 19805571
HeLa Antiviral assay 72 hrs Antiviral activity against wild type HIV1 infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay, EC50=0.016μM. 19805571
HeLa Antiviral assay 72 hrs Antiviral activity against HIV1 harboring spacer peptide A1V mutant protein infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay, EC50=0.038μM. 19805571
cord blood mononuclear cells Antiviral assay 48 hrs Antiviral activity against wild type HIV1 subtype C infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay, EC50=0.00167μM. 20404123
cord blood mononuclear cells Antiviral assay 48 hrs Antiviral activity against wild type HIV1 subtype CRF02_AG infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay, EC50=0.0057μM. 20404123
cord blood mononuclear cells Antiviral assay 48 hrs Antiviral activity against wild type HIV1 subtype B infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay, EC50=0.0098μM. 20404123
cord blood mononuclear cells Antiviral assay 48 hrs Antiviral activity against HIV1 subtype CRF02_AG harboring protease polymorphism at I36 position and M46 mutant gene infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay, EC50=0.055μM. 20404123
cord blood mononuclear cells Antiviral assay 48 hrs Antiviral activity against HIV1 subtype CRF02_AG harboring protease L33I, M46I, A71T mutant gene and polymorphism at M36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporte, EC50=0.202μM. 20404123
cord blood mononuclear cells Antiviral assay 48 hrs Antiviral activity against HIV1 subtype C harboring protease L23I, M46I, L89T mutant gene and polymorphism at M36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene , EC50=0.272μM. 20404123
cord blood mononuclear cells Antiviral assay 48 hrs Antiviral activity against HIV1 subtype B harboring protease D30N, M46I, A71T and V77I mutant gene and polymorphism at M36 position of protease infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luci, EC50=1.139μM. 20404123
cord blood mononuclear cells Antiviral assay 48 hrs Antiviral activity against HIV1 subtype B harboring protease D30N, L33I, M46I, N88D mutant gene and polymorphism at I36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter, EC50=1.463μM. 20404123
cord blood mononuclear cells Antiviral assay 48 hrs Antiviral activity against HIV1 subtype C harboring protease D30N, E35G, I85V, L90M mutant gene and polymorphism at I36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter, EC50=3.473μM. 20404123
TZM-bl Antiviral assay 48 hrs Antiviral activity against HIV1 subtype B harboring protease polymorphism at M36 position infected in human TZM-bl cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay 20404123
TZM-bl Antiviral assay 48 hrs Antiviral activity against HIV1 subtype CRF02_AG harboring protease polymorphism at I36 position infected in human TZM-bl cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay 20404123
TZM-bl Antiviral assay 48 hrs Antiviral activity against HIV1 subtype B harboring protease polymorphism at I36 position infected in human TZM-bl cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay 20404123
MT4 Antiviral assay Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells by MTT assay, EC50=0.045μM. 20439612
MT4 Antiviral assay Antiviral activity against HIV1 expressing protease L10I/L24I/M46I/V82I/I84V mutant infected in human MT4 cells selected after 50 passages of GRL-216 by MTT assay, EC50=0.13μM. 20439612
MT4 Antiviral assay 1 uM Antiviral activity against HIV1 expressing protease L10F/M46M,I/Q61Q mutant infected in human MT4 cells selected at 1 uM of GRL-396 by MTT assay, EC50=0.22μM. 20439612
MT4 Antiviral assay 1 uM Antiviral activity against HIV1 expressing protease L10F/M46I/T91S mutant infected in human MT4 cells selected at 1 uM of GRL-246 by MTT assay, EC50=0.29μM. 20439612
MT4 Antiviral assay 5 uM Antiviral activity against HIV1 expressing protease L10F/M46I/I50V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of amprenavir by MTT assay, EC50=0.3μM. 20439612
MT4 Antiviral assay 5 uM Antiviral activity against HIV1 expressing protease L10F/M46I/I54V/V82A mutant infected in human MT4 cells selected at 5 uM of Lopinavir by MTT assay, EC50=0.32μM. 20439612
MT4 Antiviral assay 1 uM Antiviral activity against HIV1 expressing protease L10F/M46L/I50V/A71Vmutant infected in human MT4 cells selected at 1 uM of GRL-286 by MTT assay, EC50=0.37μM. 20439612
MT4 Antiviral assay 5 uM Antiviral activity against HIV1 expressing protease L10I/G48V/I54V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of saquinavir by MTT assay, EC50=0.51μM. 20439612
BESM Antitrypanosomal assay 88 hrs Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BESM cells measured after 88 hrs postinfection by HTS assay, EC50=12μM. 20547819
BESM Cytotoxicity assay 88 hrs Cytotoxicity against BESM cells after 88 hrs by HTS assay, EC50=32μM. 20547819
CMEC/D3 Function assay 30 mins Inhibition of P-gp in human CMEC/D3 cells using NBD-Aba as substrate after 30 mins by flow cytometric analysis, IC50=1.7μM. 31505928
CMEC/D3 Function assay 30 mins Inhibition of P-gp in human CMEC/D3 cells using calcein-AM as substrate after 30 mins by flow cytometric analysis, IC50=2μM. 31505928
12D7-MDR Function assay 30 mins Inhibition of P-gp in human 12D7-MDR cells using NBD-Aba as substrate after 30 mins by flow cytometric analysis, IC50=5.8μM. 31505928
12D7-MDR Function assay 30 mins Inhibition of P-gp in human 12D7-MDR cells using calcein-AM as substrate after 30 mins by flow cytometric analysis, IC50=9.1μM. 31505928
12D7 Antiviral assay 3 days Antiviral activity against HIV1 LAI infected in human 12D7 cells overexpressing p-gp assessed as reduction in P24 level at 1:1 ratio of test compound to abacavir incubated for 3 days followed by followed by replacement of fresh medium containing compound 31505928
12D7 Antiviral assay 0.08 to 1.25 uM 3 days Antiviral activity against HIV1 LAI infected in human 12D7 cells overexpressing p-gp assessed as reduction in P24 level at 0.08 to 1.25 uM incubated for 3 days followed by replacement of fresh medium containing compound and measured after 3 days by ELISA 31505928
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
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
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
MT2 Antiviral assay 5 days Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as virus-induced cytopathic effect after 5 days by XTT assay, EC50=0.0049μM. ChEMBL
HepG2 Cytotoxicity assay 5 days Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 5 days by XTT assay, CC50=7.4μM. ChEMBL
skeletal myoblast cells Cytotoxicity assay 72 hours DNDI: Cytotoxicity in Vitro, 72 hour, in rat skeletal myoblast cells, IC50=12.05μM. ChEMBL
MT2 Cytotoxicity assay 5 days Cytotoxicity against human MT2 cells assessed as reduction in cell viability after 5 days by XTT assay, CC50=19.1μM. ChEMBL
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량 663.89 화학식

C33H49N3O7S2

 보관 (수령일로부터)
CAS 번호 159989-65-8 SDF 다운로드 원액 보관

동의어 AG 1343 Mesylate Smiles CC1=C(C=CC=C1O)C(=O)NC(CSC2=CC=CC=C2)C(CN3CC4CCCCC4CC3C(=O)NC(C)(C)C)O.CS(=O)(=O)O

용해도

In vitro
배치:

DMSO : 100 mg/mL (150.62 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 100 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
HIV protease
(Cell-free assay)
2 nM(Ki)
생체 내(In vivo)
생체 내 연구에 따르면 AG1343은 다양한 종에서 경구로 잘 흡수되며 인체에서 유리한 약동학적 특성을 가집니다. 사료를 먹인 쥐에 대한 화합물 초기 조사에서 경구 생체이용률이 43%로 나타났습니다. 이와 대조적으로, 금식한 쥐에서는 경구 생체이용률이 29%로 현저히 감소했습니다. Nelfinavir는 개(47%), 마모셋(17%), 게잡이원숭이(26%)를 포함한 다양한 종에서 상당한 경구 생체이용률을 보였습니다. 경구 투여 후 긴 혈장 반감기를 가지는데, 이는 느린 용해 및 흡수의 복합적인 요인 때문일 가능성이 높습니다. Nelfinavir는 특히 음식과 함께 투여할 때 사람에게 잘 흡수되며 최소한의 관리하기 쉬운 부작용을 가집니다.
참조

적용 분야

방법 바이오마커 이미지 PMID
Growth inhibition assay Cell viability
S4282-viability1
22271897
Western blot p-eIF2Aα / eIF2Aα / ATF4 / GRP78 / CHOP SOD1 / SOD2 / catalase PAX3 / MITF
S4282-WB1
21697087
Immunofluorescence LC3 / p62 PAX3 / MITF p-SMAD2
S4282-IF1
27330277

임상시험 정보

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

NCT 번호 모집 조건 스폰서/협력자 시작일 단계
NCT00051844 Completed
Human Immunodeficiency Virus
Pfizer
 August 2002 Phase 2

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