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BMS-626529 (Temsavir) is a potent HIV-1 attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4(+) T cells. BMS-626529 had half-maximal effective concentration (EC(50)) values of <10 nM against the vast majority of viral isolates. BMS-626529 exhibits an average EC50 against LAI virus of 0.7±0.4 nM. BMS-626529 exhibits an EC50 of 0.01 nM against the most susceptible virus and an EC50 of >2,000 nM against the least susceptible virus. BMS-626529 exhibits a broad spectrum of antiviral activity against a panel of clinical isolates, with an IC50 ranging from subnanomolar levels to >0.1 µM.
| Cell Experiment | |
|---|---|
| Cell lines | PBMCs |
| Preparation method | 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. |
| Concentrations | |
| Incubation time | 6 days |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 473.48 |
| Formula | C24H23N7O4 |
| CAS Number | 701213-36-7 |
| Solubility (25°C) | DMSO: 10 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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