SCH 503034 Inhibitor CAS No. 394730-60-0

Cat. No.	Name	Size	Price	Add Cart
KI0448	SCH 503034	10 mg	$772.2

Chemical Characteristic

Product Name	SCH 503034
Synonyms	Boceprevir
CAS No.	394730-60-0
Molecular Weight	519.69
Formula	C₂₇H₄₅N₅O₅
Chemical Name	(1R,2S,5S)-N-(4-amino-1-cyclobutyl-3,4-dioxobutan-2-yl)-3-[(2S)-2-(tert-butylcarbamoylamino)-3,3-dimethylbutanoyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
Smiles	[C@@H]12[C@H](N(C[C@@H]1C2(C)C)C(=O)[C@H](C(C)(C)C)NC(=O)NC(C)(C)C)C(=O)NC(CC1CCC1)C(=O)C(=O)N
Chemical Structure

Biological activities

SCH 503034 is a novel and potent oral hepatitis C virus (HCV) NS3 protease inhibitor.^[1] SCH 503034 enhances the antiviral activity of alpha interferon in replicon cells by inhibiting hepatitis C virus NS3 protease and polyprotein maturation in a mechanism-based fashion. SCH 503034 is characteristic of ketoamide inhibitors of serine proteases. SCH 503034 inhibits the single-chain NS3 protease, in a time-dependent manner, with a Ki of 14 nM. The half life (t_{1/2) for reactivation of the inhibited enzyme is 23 hours. SCH 503034 binds to the active site of the protease in a manner analogous to the C terminus of the NS3 helicase. EC50 and EC90 for SCH 503034 against Huh-7 cells with HCV are 200 and 400 nM, respectively. SCH 503034 at the dose of 400 nM reveals barely detectable levels of NS3 protein at the end of 72 hours, compared with vehicle-treated control. SCH 503034 rapidly exerts its role with effects becoming detectable in as little as 1 hour. SCH 503034 displays no toxicity by MTS on either replicon-bearing or parental Huh-7 cell lines at 50 μM after 96 hours. ^[2] Combination therapy with SCH 503034 and PEG-IFN-α-2b is well tolerated.^[1]}

Protocols

A 10 mM stock of SCH 503034 in DMSO is used to prepare serial two fold dilutions in DMSO. ^[2]

References

[1] Sarrazin C,et al. SCH 503034, a novel hepatitis C virus protease inhibitor, plus pegylated interferon alpha-2b for genotype 1 nonresponders. Gastroenterology. 2007, 132(4): 1270-1278. [2] Malcolm BA, et al. SCH 503034, a mechanism-based inhibitor of hepatitis C virus NS3 protease, suppresses polyprotein maturation and enhances the antiviral activity of alpha interferon in replicon cells. Antimicrob Agents Chemother. 2006, 50(3): 1013-1020.

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