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PSI-7976 Sale

(Synonyms: 索非布韦R-磷酸盐) 目录号 : GC37032

PSI-7976是PSI-7977的同分异构体,能抑制HCV RNA复制,EC50为1.07uM。

PSI-7976 Chemical Structure

Cas No.:1190308-01-0

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1mg
¥1,172.00
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5mg
¥8,820.00
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10mg 待询 待询
50mg 待询 待询

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Sample solution is provided at 25 µL, 10mM.

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产品描述

PSI-7976 is the isomer of PSI-7977. PSI-7977 is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.

PSI-7851 is a mixture of two diastereoisomers, PSI-7976 and PSI-7977, with PSI-7977 being the more active inhibitor of HCV RNA replication in the HCV replicon assay. Carboxylesterase 1 (CES1) preferentially hydrolyzes PSI-7976 over PSI-7977. The kinetic data also indicates that PSI-7976 is a better substrate for CES1 than for cathepsin A (CatA)[1]

[1]. Murakami E, et al. Mechanism of activation of PSI-7851 and its diastereoisomer PSI-7977. J Biol Chem. 2010 Nov 5;285(45):34337-47.

Chemical Properties

Cas No. 1190308-01-0 SDF
别名 索非布韦R-磷酸盐
Canonical SMILES O=[P@](N[C@@H](C)C(OC(C)C)=O)(OC[C@@H]1[C@@H](O)[C@](F)(C)[C@H](N2C=CC(NC2=O)=O)O1)OC3=CC=CC=C3
分子式 C22H29FN3O9P 分子量 529.45
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.8888 mL 9.4438 mL 18.8875 mL
5 mM 0.3778 mL 1.8888 mL 3.7775 mL
10 mM 0.1889 mL 0.9444 mL 1.8888 mL
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Research Update

Mechanism of activation of PSI-7851 and its diastereoisomer PSI-7977

J Biol Chem 2010 Nov 5;285(45):34337-47.PMID:20801890DOI:PMC2966047

A phosphoramidate prodrug of 2'-deoxy-2'-α-fluoro-β-C-methyluridine-5'-monophosphate, PSI-7851, demonstrates potent anti-hepatitis C virus (HCV) activity both in vitro and in vivo. PSI-7851 is a mixture of two diastereoisomers, PSI-7976 and PSI-7977, with PSI-7977 being the more active inhibitor of HCV RNA replication in the HCV replicon assay. To inhibit the HCV NS5B RNA-dependent RNA polymerase, PSI-7851 must be metabolized to the active triphosphate form. The first step, hydrolysis of the carboxyl ester by human cathepsin A (CatA) and/or carboxylesterase 1 (CES1), is a stereospecific reaction. Western blot analysis showed that CatA and CES1 are both expressed in primary human hepatocytes. However, expression of CES1 is undetectable in clone A replicon cells. Studies with inhibitors of CatA and/or CES1 indicated that CatA is primarily responsible for hydrolysis of the carboxyl ester in clone A cells, although in primary human hepatocytes, both CatA and CES1 contribute to the hydrolysis. Hydrolysis of the ester is followed by a putative nucleophilic attack on the phosphorus by the carboxyl group resulting in the spontaneous elimination of phenol and the production of an alaninyl phosphate metabolite, PSI-352707, which is common to both isomers. The removal of the amino acid moiety of PSI-352707 is catalyzed by histidine triad nucleotide-binding protein 1 (Hint1) to give the 5'-monophosphate form, PSI-7411. siRNA-mediated Hint1 knockdown studies further indicate that Hint1 is, at least in part, responsible for converting PSI-352707 to PSI-7411. PSI-7411 is then consecutively phosphorylated to the diphosphate, PSI-7410, and to the active triphosphate metabolite, PSI-7409, by UMP-CMP kinase and nucleoside diphosphate kinase, respectively.