Telaprevir Inhibitor CAS No. 402957-28-2

Cat. No.	Name	Size	Price
KI0371	Telaprevir	10 mg	$445.5
	Telaprevir	100 mg	$1782
	Telaprevir	500 mg	$3564

Chemical Characteristic

Product Name	Telaprevir
Synonyms	VX-950, INCIVEK
CAS No.	402957-28-2
Molecular Weight	679.85
Formula	C₃₆H₅₃N₇O₆
Chemical Name	(1S,3aR,6aS)-2-((S)-2-((S)-2-cyclohexyl-2-(pyrazine-2-carboxamido)acetamido)-3,3-dimethylbutanoyl)-N-((S)-1-(cyclopropylamino)-1,2-dioxohexan-3-yl)-octahydrocyclopenta[c]pyrrole-1-carboxamide
Smiles	N1([C@@H]([C@@H]2[C@H](C1)CCC2)C(=O)N([C@@H](CCC)C(=O)C(=O)NC1CC1)C(=O)C(N)C(C)(C)C)C(=O)C(NC(=O)c1cnccn1)C1CCCCC1
Chemical Structure

Biological activities

Telaprevir prevents the hepatitis C virus (HCV) protease.^[1] Telaprevir is a slow-binding peptidomimetic ketoamide inhibitor which potently inhibits the enzyme cytochrome P450 3A.^[2] Telaprevir with the HCV NS3⋅4A protease forms a weaker complex with an apparent Ki of 44 nM. After that, a rearrangement occurs. The tightly bound form of the complex of telaprevir with the HCV NS3⋅4A protease generates with a Ki of 7-10 nM. Telaprevir suppresses HCV replication with an IC50 of 0.28 μM in a genotype 1a HCV infectious virus assay. Telaprevir inhibits a genotype 1b HCV replicon with an IC50 of 0.354 μM. Telaprevir at a dose of 7 μM decreases levels of HCV replicon RNA by > 3.5-log_{10.In HCV replicon assay cells, the CC50 (50% cell kill) of telaprevir is 83 μM, resulting in an in vitro selectivity index (CC50/IC50) of 234.^[1] Telaprevir decreases levels of HCV RNA and proteins in replicon cells, in a time- and dose-dependent fashion, with a reduction of 4.7 log_{10 following a 2-week incubation. The combination of telaprevir and alpha interferon is additive to moderately synergistic in reducing HCV RNA in replicon cells with no significant increase in cytotoxicity. The benefit of the combination is sustained over time: a 4-log_{10 reduction in HCV RNA level is achieved following a 9-day incubation with telaprevir and alpha interferon at lower concentrations than when either telaprevir or alpha interferon is used alone. The combination of telaprevir and alpha interferon also suppresses the emergence of in vitro resistance mutations against telaprevir in replicon cells. The IC50s following a 24-, 48-, 72-, and 120-hour incubation with VX-950 are 0.57, 0.49, 0.21, and 0.14 μM, respectively, indicating an increase in inhibitory effects with time.^[3] In an HCV protease mouse model, telaprevir blocks HCV protease activity in the liver with an AED_{50 of < 0.3 mg/kg, and pharmacokinetic (PK) analyses establish a 6- to 16-fold higher liver-to-plasma exposure ratio 1 hour after dosing. The t_{1/2 of telaprevir is about 58 minutes.^[2]}}}}}

Protocols

Telaprevir is dissolved in 100% dimethyl sulfoxide (DMSO).^[1]

References

[1] Perni RB, et al. Preclinical profile of VX-950, a potent, selective, and orally bioavailable inhibitor of hepatitis C virus NS3-4A serine protease. Antimicrob Agents Chemother. 2006, 50(3): 899-909. [2] Garg V, et al. Effect of telaprevir on the pharmacokinetics of cyclosporine and tacrolimus. Hepatology. 2011, 54(1): 20-27. [3] Lin K, et al. VX-950, a novel hepatitis C virus (HCV) NS3-4A protease inhibitor, exhibits potent antiviral activities in HCv replicon cells. Antimicrob Agents Chemother. 2006, 50(5), 1813-1822.

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