[CAS NO. 1009119-64-5] Daclatasvir (BMS-790052)

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PRODUCTS SPECIFICATIONS [1009119-64-5]

Catalog

SLK-S1482

Brand

Selleck

CAS

1009119-64-5

DESCRIPTION [1009119-64-5]

Overview

MDL	MFCD17129086
Molecular Weight	738.88
Molecular Formula	C40H50N8O6
SMILES	C([C@@H](NC(OC)=O)C(C)C)(=O)N1[C@@H](CCC1)C=2NC(=CN2)C3=CC=C(C=C3)C4=CC=C(C=C4)C=5NC(=NC5)[C@H]6N(C([C@@H](NC(OC)=O)C(C)C)=O)CCC6

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.3534 mL	6.7670 mL	13.5340 mL
5 mM	0.2707 mL	1.3534 mL	2.7068 mL
10 mM	0.1353 mL	0.6767 mL	1.3534 mL
50 mM	0.0271 mL	0.1353 mL	0.2707 mL

Description

Daclatasvir (BMS-790052, EBP883) is a highly selective inhibitor of with of 9-50 pM, for a broad range of HCV replicon genotypes and the JFH-1 genotype 2a infectious virus in cell culture. Phase 3.

Features

First-in-class, highly selective inhibitor of hepatitis C virus (HCV) NS5A with picomolar EC50 values.

Targets

HCV NS5A ^[1]

9 pM-50 pM(EC50)

In vitro

BMS-790052 is one of the most potent inhibitors of HCV replication reported so far. The mean EC50 valuses of BMS-790052 are 50 and 9 pM for HCV genotype 1a and 1b replicons, respectively. BMS-790052 displays a therapeutic index (CC50/EC50) of at least 10 and is inactive towards a panel of 10 RNA and DNA viruses, with EC50 higher than 10 μM. This confirms BMS-790052's specificity for HCV. In Huh7 cells harboring the HCV genotype 1b replicons, BMS-790052 blocks both transient and stable HCV genome replication, with EC50 values raging from 1-15 pM. BMS-790052 (100 pM or 1 nM) has been shown to alter the subcellular localization and biochemical fractionation of NS5A. BMS-790052 inhibits hybrid replicons containing HCV genotype-4 NS5A genes with EC50 of 7-13 pM. Residue 30 of NS5A is an important site for BMS-790052-mediated resistance in the hybrid replicons.

References

[1] Gao M, et al. Nature, 2010, 465(7294), 96-100.
[2] Lee C, et al. Virology, 2011, 414(1), 10-18.
[3] Wang C, et al. Antimicrob Agents Chemother, 2012, 56(3), 1588-1590.
[4] O'Boyle DR 2nd, et al. Antimicrob Agents Chemother, 2005, 49(4), 1346-1353.

Synonyms

Carbamic acid, N,N′-[[1,1′-biphenyl]-4,4′-diylbis[1H-imidazole-5,2-diyl-(2S)-2,1-pyrrolidinediyl[(1S)-1-(1-methylethyl)-2-oxo-2,1-ethanediyl]]]bis-, C,C′-dimethyl ester

EBP 883

BMS 790052

Daclatasvir

Daklanork

Daclavirocyrl