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Daclatasvir/达拉他韦 {[allProObj[0].p_purity_real_show]}

货号:A358801 同义名: 达卡他韦 / BMS-790052; EBP 883

Daclatasvir (BMS-790052) 是一种强效和口服活性的 HCV NS5A 蛋白抑制剂,对多种 HCV 复制子基因型的 EC50 值范围为 9 至 146 pM。Daclatasvir 也是有机阴离子转运多肽 1B (OATP1B) 和 1B3 (OATP1B3) 的抑制剂,IC50 值分别为 1.5 μM 和 3.27 μM。

Daclatasvir/达拉他韦 化学结构 CAS号:1009119-64-5
Daclatasvir/达拉他韦 化学结构
CAS号:1009119-64-5
Daclatasvir/达拉他韦 3D分子结构
CAS号:1009119-64-5
Daclatasvir/达拉他韦 化学结构 CAS号:1009119-64-5
Daclatasvir/达拉他韦 3D分子结构 CAS号:1009119-64-5
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Daclatasvir/达拉他韦 纯度/质量文件 产品仅供科研

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Daclatasvir/达拉他韦 生物活性

靶点
  • HCV Protease

    HCV NS5A, EC50:9 pM-50 pM

描述 Daclatasvir is a first-in-class, highly-selective oral HCV NS5A inhibitor.

Daclatasvir/达拉他韦 细胞实验

Cell Line
Concentration Treated Time Description References
Huh7 cells 1 nM 10 days To evaluate the effect of Daclatasvir on HCV replication and assembly/secretion. Results showed that Daclatasvir treatment led to a decline in intracellular HCV RNA, similar to the polymerase inhibitor NM107, but extracellular HCV titers declined more rapidly, indicating its inhibitory effect on viral assembly/secretion. Proc Natl Acad Sci U S A. 2013 Mar 5;110(10):3991-6.
primary RDEB dermal fibroblasts 1 μM 48 h To evaluate the effect of Daclatasvir on TGF-β signaling pathway, results showed that Daclatasvir inhibited the expression of TGF-β pathway targets collagen I, phosphorylated AKT, and phosphorylated SMAD3. EMBO Mol Med. 2024 Apr;16(4):870-884.

Daclatasvir/达拉他韦 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Humanized-liver mice HBV/HCV co-infection model Oral 30 mg/kg Once a day for 4 weeks To evaluate the effect of DAA treatment on HBV replication in HBV/HCV-co-infected mice. Results showed that HCV was eliminated after DAA treatment, and HBV replication was upregulated. Sci Rep. 2020 Jan 22;10(1):941
Alb-uPA/Scid mice HCV genotype 1b or 3 infection model Oral 10 mg/kg Once daily for 4 weeks Evaluate the inhibitory effect and drug resistance of Daclatasvir monotherapy on HCV Nat Microbiol. 2020 Dec;5(12):1532-1541.
Human hepatocyte chimeric TK-NOG mice HCV infection model Oral 30 mg/kg Once daily for 4 weeks To assess the origin of HCV NS5A L31V-Y93H double substitutions after treatment failure with daclatasvir and asunaprevir combination therapy Sci Rep. 2017 Jan 30;7:41660
Mice RDEB mouse model Oral (via drinking water) 30 mg/kg From conception to weaning (28 days) To evaluate the effect of Daclatasvir on fibrosis and quality of life in RDEB mice, results showed that Daclatasvir significantly improved survival, increased weight and activity, and reduced pruritus-induced hair loss. Additionally, the expression of fibrosis markers phospho-SMAD3 and collagen I was reduced in the skin. EMBO Mol Med. 2024 Apr;16(4):870-884.

Daclatasvir/达拉他韦 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
NCT02095860 Hepatitis C Phase 1 Completed - United States, Texas ... 展开 >> Healthcare Discoveries, Llc D/B/A Icon Development Solutions San Antonio, Texas, United States, 78209 收起 <<
NCT02531269 - Completed - Switzerland ... 展开 >> Local Institution Basel, Switzerland 收起 <<
NCT03186313 Hepatitis C Phase 3 Completed - Egypt ... 展开 >> Egyptian Liver Hospital Shirbīn, Dakahlia, Egypt, 35681 收起 <<

Daclatasvir/达拉他韦 参考文献

[1]Lee C, Ma H, et al. The hepatitis C virus NS5A inhibitor (BMS-790052) alters the subcellular localization of the NS5A non-structural viral protein. Virology. 2011 May 25;414(1):10-8.

[2]Gao M, Nettles RE, et al. Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect. Nature. 2010 May 6;465(7294):96-100.

Daclatasvir/达拉他韦 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.35mL

0.27mL

0.14mL

6.77mL

1.35mL

0.68mL

13.53mL

2.71mL

1.35mL

Daclatasvir/达拉他韦 技术信息

CAS号1009119-64-5
分子式C40H50N8O6
分子量 738.88
SMILES Code O=C([C@@H](NC(OC)=O)C(C)C)N1CCC[C@H]1C2=NC=C(N2)C3=CC=C(C=C3)C4=CC=C(C5=CN=C([C@@H]6CCCN6C([C@@H](NC(OC)=O)C(C)C)=O)N5)C=C4
MDL No. MFCD17129086
别名 达卡他韦 ;BMS-790052; EBP 883
运输蓝冰
InChI Key OVPGYLMBPQNZNE-GJVQWJCYSA-N
Pubchem ID 66575053
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

DMSO: 40 mg/mL(54.14 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
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