location： Home > Products > Signaling Pathways > Proteases > HCV Protease

Daclatasvir (BMS790052; EBP883)

Price：

Market Price：

This product is for research use only, not for human use. We do not sell to patients.

Number： - + Pieces（InventoryPieces）

InvivoChem Cat #: V0724

CAS #: 1009119-64-5 (free base)Purity ≥98%

Description: Daclatasvir (formerly BMS-790052; EBP-883; trade name Daklinza), a direct-acting antiviral agent, is a selective inhibitor of HCV NS5A (nonstructural protein) with an EC50 of 9-50 pM. Daclatasvir has been used in combination with another antiviral drug (sofosbuvir) for the treatment of hepatitis C (HCV) by causing a decrease in serum HCV RNA levels. It is was developed by BMS and was approved in EU in 2014. Daclatasvir inhibits the HCV nonstructural protein NS5A. Recent study suggests that it targets two steps of the viral replication process, enabling rapid decline of HCV RNA. Daclatasvir has been tested in combination regimens with pegylated interferon and ribavirin, as well as with other direct-acting antiviral agents including asunaprevir and sofosbuvir.

References: Nature. 2010 May 6;465(7294):96-100; Virology. 2011 May 25;414(1):10-8; Antimicrob Agents Chemother. 2012 Mar;56(3):1588-90.

Related CAS: 1009119-64-5 (free base); 1009119-65-6 (Di-HCl)

Customer Validation

Top Publications Citing Invivochem Products

详情页公告 Product Catalog 2022

Bulletin Board

详情页公告 Guide to Product Handling

Publications Citing InvivoChem Products

Physicochemical and Storage Information
Protocol
Quality Control Documentation
Related Biological Data
Customer Review

Molecular Weight (MW)	738.88
Formula	C40H50N8O6
CAS No.	1009119-64-5 (free base);
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 148 mg/mL (200.3 mM)
	Water: <1 mg/mL
	Ethanol: 148 mg/mL (200.3 mM)
SMILES Code	O=C(N1CCC[[email protected]]1C2=NC=C(C3=CC=C(C4=CC=C(C=C4)C5=CN=C(N5)[[email protected]@H]6CCCN6C([[email protected]](C(C)C)NC(OC)=O)=O)C=C3)N2)[[email protected]](C(C)C)NC(OC)=O
Synonyms	BMS-790052; Daclatasvir; BMS790052; BMS 790052; EBP883; EBP 883; EBP-883; Daklinza (trade name) Chemical Name: Dimethyl N,N'-(biphenyl-4,4'-diylbis{1H-imidazole-5,2-diyl-((2S)-pyrrolidine-2,1- diyl)((1S)-1-(1-methylethyl)-2-oxoethane-2,1-diyl)})dicarbamate InChi Key: PKWSHAGFKLUEIY-CUPIEXAXSA-N InChi Code: InChI=1S/C40H50N8O6/c1-23(2)33(37(49)45-39(51)53-5)47-19-7-9-31(47)35-41-21-29(43-35)27-15-11-25(12-16-27)26-13-17-28(18-14-26)30-22-42-36(44-30)32-10-8-20-48(32)34(24(3)4)38(50)46-40(52)54-6/h11-18,21-24,31-34H,7-10,19-20H2,1-6H3,(H,41,43)(H,42,44)(H,45,49,51)(H,46,50,52)/t31-,32-,33-,34-/m0/s1

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
- Mass
- Concentration
- Volume
- Molecular Weight *
- =
- ×
- ×
The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂
- Concentration _(start)
- ×
- Volume _(start)
- =
- Concentration _(final)
- ×
- Volume _(final)
- ×
- =
- ×
- C1
- V1
- C2
- V2

In Vitro	In vitro activity: 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 105 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. Kinase Assay: Daclatasvir is a potent HCV NS5A protein inhibitor, with mean EC50 values of 50 and 9 pM against genotype 1a and 1b replicons, respectively. Cell Assay: The antiviral activity of daclatasvir towards genotypes was assessed by using replication-competent 1a or 1b replicons to construct hybrids in which the entire NS5A coding region or the first 100 amino acids of NS5A from different genotypes replaced the corresponding sequence of the parent replicon. Daclatasvir was reported to be highly potent across all HCV genotypes with half-maximum effective concentrations (EC50) ranging from 9 to 146 pM
In Vivo	Humanized liver chimeric mice, whose chimeric rate of the liver is estimated as over 40 %, are injected intravenously with 100 µL of HCV-positive human serum samples. After inoculation, their blood is collected from an external jugular vein every 1-4 weeks. The HCV RNA levels are measured by the COBAS TaqMan HCV test in 100-fold diluted serum with a lower measurement range of 3.2 log IU/mL serum. After serum levels of HCV RNA reach plateau levels, mice are administered orally once a day for 4 weeks with one of the following: 40 mg/kg of Asunaprevir plus 30 mg/kg of Daclatasvir, 15 mg/kg of Ledipasvir plus 50 mg/kg of GS-558093 and 50 mg/kg of GS-558093 plus 400 mg/kg of Telaprevir.
Animal model	Mice
Formulation & Dosage	30 mg/kg; oral
References	Nature. 2010 May 6;465(7294):96-100; Virology. 2011 May 25;414(1):10-8; Antimicrob Agents Chemother. 2012 Mar;56(3):1588-90.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Purity ≥98%
COA
MSDS

BMS-790052 alters the subcellular fractionation patterns of NS proteins. Virology. 2011 May 25;414(1):10-8.	BMS-790052 alters the subcellular localization of NS viral proteins. Virology. 2011 May 25;414(1):10-8.	BMS-790052 blocks HCV genome replication. Virology. 2011 May 25;414(1):10-8.
Reversal of BMS-790052-induced alterations on subcellular localization of NS proteins expressed from a replicon containing the BMS-790052-resistant mutation (Y93H) in NS5A. Virology. 2011 May 25;414(1):10-8.	BMS-790052 affects neither the in vitro replicase activity of pre-assembled RCs nor the self-dimerization of NS5A proteins. Virology. 2011 May 25;414(1):10-8.

Home Prev Next Last page / pices

发评论

Your information is safe with us. * Required Fields.

Product name

Cat

Applicant name

Email address

Phone number

Organization name

Country

Requested quantity

Remarks