Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate) is a potent, selective, oral bioavailable and CNS penetrated antagonist of CCR5, with a Ki of 2.5 nM, and also inhibits HIV-1 in PBMC cells, with IC90s of 3.3 nM (JrFL), 2.8 nM (ADA-M), 1.8 nM (301657), 4.9 nM (JV1083) and 10 nM (RU 570).
Molecular Weight | 649.7 |
Formula | C32H42F3N5O6 |
CAS Number | 599179-03-0 |
Form | Solid |
Solubility (25°C) | DMSO 50 mg/mL (ultrasonic) Water 25 mg/mL (Need ultrasonic and warming) |
Storage | 4°C, dry, sealed |
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] A Tomillero, et al. Methods Find Exp Clin Pharmacol. Gateways to clinical trials
[2] A Tomillero, et al. Methods Find Exp Clin Pharmacol. Gateways to clinical trials
[3] A Tomillero, et al. Methods Find Exp Clin Pharmacol. Gateways to clinical trials
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