Daclatasvir dihydrochloride
(Synonyms: 盐酸达拉他韦; BMS-790052 dihydrochloride; EBP 883 dihydrochloride) 目录号 : GC12236
An NS5A inhibitor
Cas No.:1009119-65-6
Sample solution is provided at 25 µL, 10mM.
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BMS-790052 is a potent inhibitor of HCV NS5A with EC50 value of 9-50 pM [1].
NS5A (nonstructural protein 5A) is a zinc-binding protein and plays a pivotal role in HCV RNA replication. NS5A involves in mediating the host cell function and HCV infection, therefore, it is regarded as a promising target for HCV treatment [2].
BMS-790052 is a selective HCV NS5A inhibitor and has the most potent ability to inhibit HCV replication reported so far. When using FRET assays to determine the efficiay of BMS-790052 on HCV NS5A, replicon cells were cultured in 96-well plates and after 12 hours BMS-790052 was added to test the replication activity and cytotoxicity, the results showed that the mean values of BMS-790052 for genotype 1a and 1b were 50 and 9 pM, respectively [1]. In stable replication cell lines with GT-5a hybrid replicons (GT-5a-6, GT-5a-7, and GT-5a-9), BMS-790052 treatment showed effective antiviral activity with EC50 values range from 3 to 7 pM [3].
It has been shown that oral administration of BMS-790052 was safe and well tolerated up to 200 mg when tested with healthy people, and it was safe and well tolerated at the dose of 100 mg when tested with HCV-infected patients [1].
References:
[1]. Gao, M., et al., Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect. Nature, 2010. 465(7294): p. 96-100.
[2]. Eyre, N.S. and M.R. Beard, HCV NS5A inhibitors disrupt replication factory formation: a novel mechanism of antiviral action. Gastroenterology, 2014. 147(5): p. 959-62.
[3]. Wang, C., et al., Comparison of daclatasvir resistance barriers on NS5A from hepatitis C virus genotypes 1 to 6: implications for cross-genotype activity. Antimicrob Agents Chemother, 2014. 58(9): p. 5155-63.
| Cas No. | 1009119-65-6 | SDF | |
| 别名 | 盐酸达拉他韦; BMS-790052 dihydrochloride; EBP 883 dihydrochloride | ||
| 化学名 | dimethyl ((2S,2'S)-((2S,2'S)-2,2'-(5,5'-([1,1'-biphenyl]-4,4'-diyl)bis(1H-imidazole-5,2-diyl))bis(pyrrolidine-2,1-diyl))bis(3-methyl-1-oxobutane-2,1-diyl))dicarbamate dihydrochloride | ||
| Canonical SMILES | CC(C)[C@H](NC(OC)=O)C(N1[C@H](C2=NC=C(C3=CC=C(C4=CC=C(C5=CN=C([C@@H]6CCCN6C([C@@H](NC(OC)=O)C(C)C)=O)N5)C=C4)C=C3)N2)CCC1)=O.Cl.Cl | ||
| 分子式 | C40H52Cl2N8O6 | 分子量 | 811.8 |
| 溶解度 | DMSO : 100mg/mL; Water : 100mg/mL | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.2318 mL | 6.1592 mL | 12.3183 mL |
| 5 mM | 0.2464 mL | 1.2318 mL | 2.4637 mL |
| 10 mM | 0.1232 mL | 0.6159 mL | 1.2318 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet