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CAS No.: 1009119-65-6

Daclatasvir 2HCl/盐酸达拉他韦 Catalog No. CSN12832

Synonyms: BMS-790052 dihydrochloride;EBP 883 dihydrochloride;BMS-790052 2HCl

Daclatasvir 2HCl is a selective HCV NS5A inhibitor with EC50 of 9 pM - 50 pM.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 HCV NS5A

EC50:9-50pM
描述Hepatitis C virus (HCV) is a positive-strand RNA virus belonging to the family Flaviviridae. The viral proteins required for RNA replication include NS3, NS4A, NS4B, NS5A, and NS5B. NS5A has been shown to interact with a number of host proteins, is implicated in interferon resistance in vivo^[3]. Daclatasvir Dihydrochloride is a small molecule inhibitor of the HCV NS5A protein with EC₅₀ values ranging from 9 to 146 pM towards all genotypes tested. More significantly, daclatasvir is a potent inhibitor of the JFH-1 genotype 2a infectious virus that replicates in cell culture (EC₅₀ = 28 pM). In addition, daclatasvir displayed similar potency in Huh-7, HeLa and HEK293T cells. In a randomized, double-blind, placebo-controlled study, the EC₉₀ for daclatasvir is 383 pM for the genotype 1a replicon and 49 pM for the genotyope 1b replicon in the presence of 40% human serum^[4]. In a mouse model of HCV replication, daclatasvir administered alone perorally (once a day at 30 mg/kg body weight) reduced serum HCV RNA titers very rapidly by ~1.5 log₁₀ at day 3, proving its superior anti-HCV efficacy^[5].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03748745	Drug Interactions	Phase 1	Active, not recruiting	January 19, 2019	China, Jilin ... more >> Phase I Clinical Trial Unit, The First Hospital of Jilin University Changchun, Jilin, China, 130000 Collapse <<

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.2318 mL
- 6.1592 mL
- 12.3184 mL
- 5 mM
- 0.2464 mL
- 1.2318 mL
- 2.4637 mL
- 10 mM
- 0.1232 mL
- 0.6159 mL
- 1.2318 mL

技术信息

CAS号

1009119-65-6

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C40H52Cl2N8O6

运输

蓝冰

分子量

811.80

别名

BMS-790052 dihydrochloride;EBP 883 dihydrochloride;BMS-790052 2HCl;Daclatasvir HCl;Daclatasvir 2HCl;BMS-790052;EBP-883;trade name Daklinza;盐酸达拉他韦

溶解度

DMSO	50.0 mg/mL (61.6 mM) warming
Water	100.0 mg/mL (123.2 mM) warming

动物实验配方

0.5% CMC-Na

40 mg/mL

suspension

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