Valopicitabine dihydrochloride
(Synonyms: NM283 dihydrochloride) 目录号 : GC63635
Valopicitabine (NM283) dihydrochloride 是一种核苷类似物，是强效抗 HCV 剂的 2’-C-甲基胞苷 (NM107) 的口服生物利用前药。NM107 竞争性抑制 NS5B 聚合酶，导致链终止。
Cas No.:640725-71-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Valopicitabine (NM283) dihydrochloride is a nucleoside analog and the orally bioavailable prodrug of the potent anti-HCV agent 2’-C-methylcytidine (NM107). NM107competitively inhibits NS5B polymerase, causing chain termination[1][2].
Valopicitabine (NM283) (100 mg/kg; oral administration; Sprague-Dawley Rats) dihydrochloride shows the Cmax, AUC, t1/2, and tmax were 3.624 μg/mL, 8.95 μg h/mL, 0.64 hours and 1 hour, respectively[2].
[1]. Liu-Young G, et al. Hepatitis C protease and polymerase inhibitors in development. AIDS Patient Care STDS. 2008;22(6):449-457.
[2]. Pierra C, et al. Synthesis and pharmacokinetics of valopicitabine (NM283), an efficient prodrug of the potent anti-HCV agent 2’-C-methylcytidine. J Med Chem. 2006;49(22):6614-6620.
| Cas No. | 640725-71-9 | SDF | |
| 别名 | NM283 dihydrochloride | ||
| 分子式 | C15H26Cl2N4O6 | 分子量 | 429.3 |
| 溶解度 | H2O : 100 mg/mL (232.94 mM; Need ultrasonic); DMSO : 100 mg/mL (232.94 mM; Need ultrasonic) | 储存条件 | Store at -20°C, protect from light, stored under nitrogen |
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3294 mL | 11.6469 mL | 23.2937 mL |
| 5 mM | 0.4659 mL | 2.3294 mL | 4.6587 mL |
| 10 mM | 0.2329 mL | 1.1647 mL | 2.3294 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。
Valopicitabine dihydrochloride:a specific polymerase inhibitor of hepatitis C virus
Curr Opin Investig Drugs 2007 Feb;8(2):150-8.PMID:17328231doi
Idenix Pharmaceuticals Inc and Novartis AG are codeveloping Valopicitabine dihydrochloride, a once-daily oral nucleoside for the potential treatment of HCV infection. In January 2005, a phase IIa clinical trial comparing Valopicitabine dihydrochloride with pegylated IFN in treatment-naive HCV patients was ongoing, in addition to a phase IIb trial in patients that had previously failed pegylated IFN and ribavirin combination therapy. In January 2006, an international phase III trial in treatment-refractory patients was planned for the first half of the year, with a phase III trial in treatment-naive individuals planned for the second half of the year.