| Description | Temsavir (BMS626529) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+ T cells. |
| In vitro | Temsavir的半最大有效浓度（EC50）值对绝大多数病毒分离物均2,000 nM。在不同人体组织的几种细胞类型中检查了Temsavir的细胞毒性概况。在培养3或6天后，观察到MT-2（T淋巴细胞）、HEK293（肾）、HEp-2（喉）、HepG2（肝）、HeLa（宫颈）、HCT116（结直肠）、MCF-7（乳腺）、SK-N-MC（神经上皮）、HOS（骨）、H292（肺）和MDBK（牛肾）细胞中的CC50值>200 μM。在6天的培养后，T细胞系PM1和PBMCs分别获得105和192 μM的CC50值。这些结果表明Temsavir在细胞培养中表现出低细胞毒性。Temsavir针对一系列临床分离物展现出广谱的抗病毒活性，50%抑制浓度（IC50）范围从亚nM级别到>0.1 μM。 |
| Cell experiments | Cytotoxicity assays are performed in the presence of serially diluted BMS-626529 for up to 6 days, and cell viability is quantitated using an XTT assay. To determine CC50?values (concentration of drug required to kill 50% of cells), laboratory-adapted peripheral blood mononuclear cells (PBMCs) are initially plated at a density of 0.1×106?cells/mL. In the absence of compounds, the cell densities typically reach 1×106?to 1.2×106/mL after 6 days[1]. |
| Synonyms | BMS626529 |
| molecular weight | 473.48 |
| Molecular formula | C24H23N7O4 |
| CAS | 701213-36-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 8.57 mg/mL (18.1 mM), Sonication is recommended. |
| References | 1. Nowicka-Sans B, et al. In vitro antiviral characteristics of HIV-1 attachment inhibitor BMS-626529, the active component of the prodrug BMS-663068. Antimicrobial Agents and Chemotherapy (2012), 56(7), 3498-3507. 2. Nettles RE, et al. Pharmacodynamics, safety, and pharmacokinetics of BMS-663068, an oral HIV-1 attachment inhibitor in HIV-1-infected subjects. J Infect Dis. 2012 Oct 1;206(7):1002-11. |