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 | |
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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 | |
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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 |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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