Balapiravir
(Synonyms: 4'-C-迭氮基胞嘧啶核苷2',3',5'-三异丁酸酯,R-1626; R1626; Ro 4588161;R1626;Ro4588161;Ro-4588161) 目录号 : GC10930Balapiravir (Ro 4588161; R1626) 是 HCV (R1479; 4'-Azidocytidine) 的 RNA 依赖性 RNA 聚合酶 (RdRp) 的核苷类似物抑制剂的口服活性前药。
Cas No.:690270-29-2
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Balapiravir (R1626, Ro 4588161) is the prodrug of a nucleoside analogue inhibitor of the hepatitis C virus (HCV) RNA-dependent RNA polymerase (R1479, RG1479).IC50 Value: Target: HCVBalapiravir(R-1626; R 1626; Ro 4588161) is useful for Anti HCV. Balapiravir (R1626) is the tri-isobutyrate ester prodrug of R1479 under clinical development to improve exposure of R1479 upon oral administration. Balapiravir was discontinued for safety reasons in 28-36% of patients (most often for lymphopenia) and the percentage of patients with serious adverse events (especially hematological, infection, ocular events) was dose related. Serious hematological adverse events (particularly neutropenia, lymphopenia) were more common in balapiravir recipients. Two deaths in the balapiravir/peginterferon alfa-2a/ribavirin combination groups were considered possibly related to study medication.
References:
[1]. Nguyen NM, et al. A randomized, double-blind placebo controlled trial of balapiravir, a polymerase inhibitor, in adult dengue patients. J Infect Dis. 2013 May 1;207(9):1442-1450.
[2]. Nelson DR, et al. Balapiravir plus peginterferon alfa-2a (40KD)/ribavirin in a randomized trial of hepatitis C genotype 1 patients.Ann Hepatol. 2012 Jan-Feb;11(1):15-31.
[3]. Li F, et al. Chemical stability of 4'-azidocytidine and its prodrug balapiravir.Drug Dev Ind Pharm. 2010 Apr;36(4):413-20.
[4]. kros PJ, et al. R1626 plus peginterferon Alfa-2a provides potent suppression of hepatitis C virus RNA and significant antiviral synergy in combination with ribavirin.Hepatology. 2008 Aug;48(2):385-97.
[5]. Roberts SK, et al. Robust antiviral activity of R1626, a novel nucleoside analog: a randomized, placebo-controlled study in patients with chronic hepatitis C.Hepatology. 2008 Aug;48(2):398-406.
[6]. Chen YL, et al. Activation of peripheral blood mononuclear cells by dengue virus infection depotentiates balapiravir. J Virol. 2014 Feb;88(3):1740-1747.
Cas No. | 690270-29-2 | SDF | |
别名 | 4'-C-迭氮基胞嘧啶核苷2',3',5'-三异丁酸酯,R-1626; R1626; Ro 4588161;R1626;Ro4588161;Ro-4588161 | ||
化学名 | [(2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-2-azido-3,4-bis(2-methylpropanoyloxy)oxolan-2-yl]methyl 2-methylpropanoate | ||
Canonical SMILES | CC(C)C(=O)OCC1(C(C(C(O1)N2C=CC(=NC2=O)N)OC(=O)C(C)C)OC(=O)C(C)C)N=[N+]=[N-] | ||
分子式 | C21H30N6O8 | 分子量 | 494.5 |
溶解度 | Soluble in DMSO | 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.0222 mL | 10.1112 mL | 20.2224 mL |
5 mM | 0.4044 mL | 2.0222 mL | 4.0445 mL |
10 mM | 0.2022 mL | 1.0111 mL | 2.0222 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 | ||||||||||
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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。