BMS-663068 is the phosphonooxymethyl prodrug of BMS626529, a novel small-molecule attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+ T cells with EC50 of < 10 nM.
Molecular Weight | 583.49 |
Formula | C25H26N7O8P |
CAS Number | 864953-29-7 |
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.
[1] Michael Kozal, et al. Fostemsavir in Adults with Multidrug-Resistant HIV-1 Infection
[2] Mary C Cambou, et al. Novel Antiretroviral Agents
[3] Ester Ballana, et al. BMS-663068, a safe and effective HIV-1 attachment inhibitor
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