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Vicriviroc Malate

Cat. No. M2032

Vicriviroc Malate Structure

Synonym: SCH 417690

Size Price Availability
5mg USD 150 Out of stock
10mg USD 250 Out of stock
50mg USD 550 Out of stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 667.72
Formula C28H38F3N5O2.C4H6O5
CAS Number 541503-81-5
Purity >99%
Solubility Water
Storage at -20°C
References

Antiviral activity, pharmacokinetics and safety of vicriviroc, an oral CCR5 antagonist, during 14-day monotherapy in HIV-infected adults.
Schürmann D, et al. AIDS. 2007 Jun 19;21(10):1293-9. PMID: 17545705.

Discovery and characterization of vicriviroc (SCH 417690), a CCR5 antagonist with potent activity against human immunodeficiency virus type 1.
Strizki JM, et al. Antimicrob Agents Chemother. 2005 Dec;49(12):4911-9. PMID: 16304152.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Vicriviroc Malate, SCH 417690 supplier, CCR, inhibitors

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