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Vicriviroc Malate

Cat. No. M2032
Vicriviroc Malate Structure
Synonym:

SCH 417690

Size Price Availability Quantity
5mg USD 520  USD520 In stock
10mg USD 745  USD745 In stock
25mg USD 1520  USD1520 In stock
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Quality Control & Documentation
Biological Activity

Vicriviroc is an orally available CCR5 antagonist, which binds specifically to the CCR5 receptor and prevents infection of target cells by CCR5-tropic HIV-1 isolates. Vicriviroc potently inhibited all the viral isolates tested, with geometric mean EC50s ranging between 0.04 nM and 2.3 nM and IC90s between 0.45 nM and 18 nM. Vicriviroc inhibits MIP-1α induced migration of Ba/F3 cells stably expressing recombinant human CCR5, with IC50 of 0.91 nM. Vicriviroc inhibits GTPγS binding to the membranes from HTS-hCCR5 cells induced by RANTES, with IC50 of 4.2 nM. Competition binding assays revealed that vicriviroc binds with higher affinity to CCR5 than SCH-C. Finally, vicriviroc demonstrated diminished affinity for the human ether a-go-go related gene transcript ion channel compared to SCH-C, suggesting a reduced potential for cardiac effects.

Chemical Information
Molecular Weight 667.72
Formula C28H38F3N5O2.C4H6O5
CAS Number 541503-81-5
Solubility (25°C) Water
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Schürmann D, et al. AIDS. Antiviral activity, pharmacokinetics and safety of vicriviroc, an oral CCR5 antagonist, during 14-day monotherapy in HIV-infected adults.

[2] Strizki JM, et al. Antimicrob Agents Chemother. Discovery and characterization of vicriviroc (SCH 417690), a CCR5 antagonist with potent activity against human immunodeficiency virus type 1.

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