GSK3532795
Based on 1 Customer Validation
GSK3532795 (BMS-955176) is a potent, orally active, second-generation HIV-1 maturation inhibitor, with EC50s of 1.9, 10.2, 2.7 and 13 nM for HIV-1 WT, HIV-1 WT(human serum), HIV-1 V370A, and HIV-1 ΔV370, respectively.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.0%
- CAS 番号: 1392312-45-6
- 分子式: C42H62N2O4S
- 分子量:691.02
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
|
HIV-1 |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MT2 | CC50 |
13 μM
Compound: 3; GSK3532795, BMS-955176
|
Cytotoxicity against human MT2 cells assessed as reduction in cell viability
Cytotoxicity against human MT2 cells assessed as reduction in cell viability
|
[PMID: 36441509] |
| MT2 | CC50 |
13 μM
Compound: 4; GSK3532795, BMS-955176
|
Cytotoxicity in human MT2 cells assessed as reduction in cell viability
Cytotoxicity in human MT2 cells assessed as reduction in cell viability
|
[PMID: 36044257] |
| MT2 | CC50 |
9.2 nM
Compound: 2; BMS-955176
|
Cytotoxicity against human MT2 cells
Cytotoxicity against human MT2 cells
|
[PMID: 27326328] |
| MT2 | CC50 |
9.2 μM
Compound: 1; BMS-955176, GSK3532795
|
Cytotoxicity against human MT2 cells assessed as reduction in cell viability
Cytotoxicity against human MT2 cells assessed as reduction in cell viability
|
[PMID: 30067361] |
| MT2 | CC50 |
9.2 μM
Compound: 3; GSK3532795; BMS-955176
|
Cytotoxicity against human MT2 cells
Cytotoxicity against human MT2 cells
|
[PMID: 33508465] |
| MT2 | EC50 |
1.9 nM
Compound: 2; BMS-955176
|
Binding affinity to gag polyprotein in wild type HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein in wild type HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
|
[PMID: 27326328] |
| MT2 | EC50 |
1.9 nM
Compound: 2; BMS-955176
|
Binding affinity to gag polyprotein Q369H mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein Q369H mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
|
[PMID: 27326328] |
| MT2 | EC50 |
10.2 nM
Compound: 2; BMS-955176
|
Binding affinity to gag polyprotein in wild type HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum/40% human serum/27 mg/ml human serum albumin by dual-lucife
Binding affinity to gag polyprotein in wild type HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum/40% human serum/27 mg/ml human serum albumin by dual-lucife
|
[PMID: 27326328] |
| MT2 | EC50 |
13 nM
Compound: 2; BMS-955176
|
Binding affinity to gag polyprotein V370A deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein V370A deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
|
[PMID: 27326328] |
| MT2 | EC50 |
2 nM
Compound: 2; BMS-955176
|
Binding affinity to gag polyprotein V371A deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein V371A deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
|
[PMID: 27326328] |
| MT2 | EC50 |
2.7 nM
Compound: 2; BMS-955176
|
Binding affinity to gag polyprotein V370A mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein V370A mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
|
[PMID: 27326328] |
| MT2 | EC50 |
2.8 nM
Compound: 2; BMS-955176
|
Binding affinity to gag polyprotein V370M mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein V370M mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
|
[PMID: 27326328] |
| MT2 | EC50 |
3.6 nM
Compound: 2; BMS-955176
|
Binding affinity to gag polyprotein V370A/T371 deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein V370A/T371 deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
|
[PMID: 27326328] |
| MT2 | EC50 |
3.9 nM
Compound: 2; BMS-955176
|
Binding affinity to gag polyprotein in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation
Binding affinity to gag polyprotein in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation
|
[PMID: 27326328] |
| MT2 | EC50 |
4.5 nM
Compound: 2; BMS-955176
|
Binding affinity to gag polyprotein V3621 mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein V3621 mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
|
[PMID: 27326328] |
| MT2 | EC50 |
7.3 nM
Compound: 2; BMS-955176
|
Binding affinity to gag polyprotein T371 deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein T371 deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
|
[PMID: 27326328] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1392312-45-6
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性状 Solid
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分子量 691.02
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分子式 C42H62N2O4S
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Color White to off-white
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SMILES
CC1(C)C(C2=CC=C(C(O)=O)C=C2)=CC[C@@]3(C)[C@@]1([H])CC[C@]4(C)[C@]3([H])CC[C@@]5([H])[C@@]4(C)CC[C@]6(NCCN7CCS(CC7)(=O)=O)[C@]5([H])[C@H](C(C)=C)CC6
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別名
BMS-955176
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
純度とドキュメンテーション
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データシート (269 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Regueiro-Ren A, et al. Design, Synthesis, and SAR of C-3 Benzoic Acid, C-17 Triterpenoid Derivatives. Identification of the HIV-1 Maturation Inhibitor 4-((1 R,3a S,5a R,5b R,7a R,11a S,11b R,13a R,13b R)-3a-((2-(1,1-Dioxidothiomorpholino)ethyl)amino)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-2,3,3a,4,5,5a,5b,6,7,7a,8,11,11a,11b,12,13,13a,13b-octadecahydro-1 H-cyclopenta[ a]chrysen-9-yl)benzoic Acid (GSK3532795, BMS-955176). J Med Chem. 2018 Aug 23;61(16):7289-7313. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)