VX-222 Inhibitor CAS No. 1026785-59-0

Cat. No.	Name	Size	Price
KI0165	VX-222	5 mg	$272
	VX-222	10 mg	$512
	VX-222	50 mg	$1552
	VX-222	200 mg	$3952

Chemical Characteristic

Product Name	VX-222
Synonyms	VCH-222
CAS No.	1026785-59-0
Molecular Weight	445.61
Formula	C₂₅H₃₅NO₄S
Chemical Name	5-(3,3-dimethylbut-1-ynyl)-3-[(4-hydroxycyclohexyl)-(4-methylcyclohexanecarbonyl)amino]thiophene-2-carboxylic acid
Smiles	c1(c(cc(s1)C#CC(C)(C)C)N(C(=O)C1CC[C@@H](CC1)C)C1CC[C@H](CC1)O)C(=O)O
Chemical Structure

Biological activities

VX-222 is a NS5B (a RNA dependent RNA polymerase of Hepatitis C virus) non-nucleoside polymerase inhibitor.^[1] The EC50 of VX-222 is 22.3, 11.2 and 2.6 nM against HCV (hepatitis C virus) sub-genomic replicon genotype 1a, 1b and 2a, respectively.^[2] In addition, VX-222 inhibits HCV NS5B genotypes 1a, 1b and 2a with IC50 of 0.94, 1.2 and 12.3 µM, respectively. As described above, VX-222 has a potent in vitro activity against HCV NS5B genotype 1a and 1b with low micromolar IC50. However, a 10-fold reduction in potency is observed when tested against HCV NS5B genotype 2a. VX-222 also inhibits DNA polymerase ? with an IC50 of 56 µM. The potency of VX-222 in the replicon assay is affected by the presence of human serum albumin which is consistent with the high binding affinity of VX-222 to human plasma proteins. VX-222 has an in vitro therapeutic index of ∼4000 indicating a high anti-HCV specific activity.^[3] VX-222 inhibits the 1b/Con1 HCV subgenomic replicon, with EC50 of 5 nM. VX-222 binds to the HCV polymerase with dissociation constant of 17 nM. ^[4] VX-222 demonstrates limited potential to cause human CYP (cytochrome P450) inhibition or CYP induction. In rats and dogs, VCH-222 reveals low total body clearance with excellent oral bioavailability (greater than 30%). The exposure of VCH-222 in rat liver is 5-fold higher than in plasma. VCH-222 is metabolically stable in human microsomes and hepatocytes. ^[5]

References

[1] Gane E. Future hepatitis C virus treatment: interferon-sparing combinations. Liver Int. 2011, 31(Suppl 1): 62-67. [2] Li H, et al. Non-nucleoside inhibitors of hepatitis C virus polymerase: current progress and future challenges. Future Med Chem. 2010, 2(1): 121-141. [3] Bedard J, et al. Identification and characterization of VCH-222, a novel potent and selective non-nucleoside HCV polymerase inhibitor. The 44th Annual Meeting of the European Association for the Study of the Liver. Copenhagen, Denmark, 22??6 April 2009. [4] Yi G, et al. Biochemical study of the comparative inhibition of hepatitis C virus RNA polymerase by VX-222 and filibuvir. Antimicrob Agents Chemother. 2012, 56(2): 830-837. [5] Chauret N, et al. Preclinical pharmacokinetic and ADME characterization of VCH-222, a novel non-nucleoside HCV NS5B polymerase inhibitor. The 44th Annual Meeting of the European Association for the Study of the Liver. Copenhagen, Denmark, 22??6 April 2009. [6] Bedard J, et al. Identification and characterization of VCH-222, a novel potent and selective non-nucleoside HCV polymerase inhibitor. The 44th Annual Meeting of the European Association for the Study of the Liver. Copenhagen, Denmark, 22??6 April 2009.

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