Cat. No. Name Size Price Add Cart
KI0374Vicriviroc Malate5 mg$490
Vicriviroc Malate10 mg$900
Vicriviroc Malate50 mg$2234

Chemical Characteristic

Product NameVicriviroc Malate
SynonymsSCH-417690, SCH-D
CAS No.541503-81-5
Molecular Weight 667.72
FormulaC32H44F3N5O7
Chemical Name1-[(4,6-Dimethyl-5-pyrimidinyl)carbonyl]-4-[(3S)-4-[(1R)-2-methoxy-1-[4-(trifluoromethyl)phenyl]ethyl]-3-methyl-1-piperazinyl]-4-methylpiperidine malate
SmilesN1(CCC(CC1)(C)N1C[C@@H](N(CC1)[C@H](COC)c1ccc(cc1)C(F)(F)F)C)C(=O)c1c(ncnc1C)C C(=O)(C(O)CC(=O)O)O
Chemical Structure

Biological activities

Vicriviroc malate is a malate salt form of vicriviroc which is a novel CCR5 antagonist. Vicriviroc binds specifically to the CCR5 receptor with a Ki of 0.8 nM. Vicriviroc prevents infection of target cells by CCR5-tropic HIV-1 isolates. In antiviral assays, vicriviroc shows potent, broad-spectrum activity against genetically diverse and drug-resistant HIV-1 isolates. Vicriviroc blocks calcium release induced by the ligand RANTES(regulated upon activation, normal T-cell expressd and secreted). Vicriviroc reveals potent inhibition of the chemotactic response to MIP-1α with IC50 of less than 0.9 nM. Vicriviroc inhibits GTPγS binding induced by RANTES with IC50 of 16 nM. Vicriviroc potently inhibits RANTES-induced signaling with IC50 of 4.2 nM. Vicriviroc has a high affinity with a Kd of 1.25 nM. [1] Vicriviroc inhibits a wide range of HIV-1 strains from various genetic subtypes with inhibitory concentrations in the low nM range. The Vicriviroc prevents CCI/85 and CC101.6 viruses with IC50 of 0.95 and 3 nM, respectively.[2] Vicriviroc potently inhibits all the viral isolates tested including 93RW023, 93RW034 with EC50 ranging from 0.04 to 2.3 nM and IC90 rainging from 0.45 to 18 nM. Vicriviroc is active against the viruses with reverse transcriptase inhibitor (RTI), protease inhibitor (PRI), or multidrug resistance (MDR) phenotypes, with EC50 comparable to those of the wild-type control virus. In addition, vicriviroc is active against both the virus containing the gp41 V38A mutation as well as the virus with the double mutation (G36D and V28M) with EC50s similar to (<2-fold) that obtained for the wild-type comparator virus. In both rats and monkeys, vicriviroc displays excellent absorption (95 to 100%) and oral bioavailability (89 to 100%), with Cmax values of 1.3 μM in monkeys receiving a dose of 2 mg per kg body weight.[1]

Protocols

The vicrivirocis dissolved in 0.4% methylcellulose for oral dosing and in 20% hydroxypropyl-β-cyclodextrin for i.v. dosing. [1]

References

[1] Strizki JM, et al. Discovery and characterization of vicriviroc (SCH 417690), a CCR5 antagonist with potent activity against human immunodeficiency virus type 1. Antimicrob Agents Chemother. 2005, 49(12): 4911-4919.
[2] Marozsan AJ, et al. Generation and properties of a human immunodeficiency virus type 1 isolate resistant to the small molecule CCR5 inhibitor, SCH-417690 (SCH-D). Virology. 2005, 338(1): 182-199.

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