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Vicriviroc maleate

Cat. No. M30343
Vicriviroc maleate Structure
Synonym:

SCH-417690 maleate; SCH-D maleate

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Biological Activity

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).

Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[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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Keywords: Vicriviroc maleate, SCH-417690 maleate; SCH-D maleate supplier, CCR, inhibitors, activators


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