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Ombitasvir

Ombitasvir

产品编号 T7158   CAS 1258226-87-7
别名: 奥比他韦, ABT-267

Ombitasvir (ABT-267) 是丙型肝炎病毒非结构蛋白 5A 的口服生物可利用的强效抑制剂。对 HCV 基因型 1 至 5 的 EC50 为 0.82 至 19.3 pM,对基因型 6a 的 EC50 为 366 pM。

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Ombitasvir Chemical Structure
Ombitasvir, CAS 1258226-87-7
规格 价格/CNY 货期 数量
1 mg ¥ 378 现货
5 mg ¥ 913 现货
10 mg ¥ 1,490 现货
25 mg ¥ 2,930 现货
50 mg ¥ 4,390 现货
100 mg ¥ 6,290 现货
500 mg ¥ 12,800 现货
1 mL * 10 mM (in DMSO) ¥ 1,460 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
MG-132限时半价
重组蛋白限时优惠
产品目录号及名称: Ombitasvir (T7158)
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纯度: 99.56%
纯度: 98.17%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Ombitasvir (ABT-267) is an orally bioavailable and potent inhibitor of the hepatitis C virus (HCV) non-structural protein 5A (NS5A).with EC50s of 0.82 to 19.3 pM against HCV genotypes 1 to 5, and 366 pM against genotype 6a
靶点活性 HCVs 1-5:0.82 pM-19.3 pM(EC50) , HCV 6a:366 pM(EC50)
体内活性 Ombitasvir was evaluated in vivo in a 3-day monotherapy study in 12 HCV genotype 1-infected patients at 5, 25, 50, or 200 mg dosed once daily. All patients were HCV genotype 1a infected and were without preexisting resistant variants at baseline as determined by clonal sequencing. Decreases in HCV RNA up to 3.1 log10 IU/ml were observed. Resistance-associated variants at position 28, 30, or 93 in NS5A were detected in patient samples 48 hours after the first dose. Clonal sequencing analysis indicated that wild-type virus was largely suppressed by ombitasvir during 3-day monotherapy, and at doses higher than 5 mg, resistant variant M28V was also suppressed. Ombitasvir was well tolerated at all doses, and there were no serious or severe adverse events. These data support clinical development of ombitasvir in combination with inhibitors targeting HCV NS3/4A protease (ABT-450 with ritonavir) and HCV NS5B polymerase (ABT-333, dasabuvir) for the treatment of chronic HCV genotype 1 infection[1].
动物实验 The patients in the ombitasvir dose groups were enrolled sequentially, and within each group, patients were randomized (2:1) to either ombitasvir or placebo and treated under nonfasting conditions for 3 days while confined to the study site. The 200-mg dose group received a different formulation with higher bioavailability. Patients who received at least one dose of ombitasvir or placebo were provided the option to receive treatment with pegIFN/RBV for approximately 48 weeks once treatment with ombitasvir was completed. HCV RNA was measured using the Roche COBAS TaqMan HCV Test v2.0 real-time reverse transcriptase PCR assay (with a lower limit of quantification of 25 IU/ml and a lower limit of detection of 10 IU/ml). The virologic response was assessed as HCV RNA decrease from baseline in log10 IU/ml[1].
别名 奥比他韦, ABT-267
分子量 894.11
分子式 C50H67N7O8
CAS No. 1258226-87-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 33 mg/mL (36.91 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1184 mL 5.5922 mL 11.1843 mL 27.9608 mL
5 mM 0.2237 mL 1.1184 mL 2.2369 mL 5.5922 mL
10 mM 0.1118 mL 0.5592 mL 1.1184 mL 2.7961 mL
20 mM 0.0559 mL 0.2796 mL 0.5592 mL 1.398 mL

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TargetMol Library Books参考文献

1. Krishnan P, Beyer J, Mistry N,et al.in vitro and in vivo antiviral activity and resistance profile of ombitasvir, an inhibitor of hepatitis c virus ns5a[J].Antimicrob Agents Chemother. 2015 Feb;59(2):979-87. 2. Keating, Gillian M . Ombitasvir/Paritaprevir/Ritonavir: A Review in Chronic HCV Genotype 4 Infection[J]. Drugs, 2016, 76(12):1203-1211.
Deapioplatycodin D ACH-806 Azvudine VCH-916 HCV-IN-29 Clemizole GS-9256 Tomeglovir

相关化合物库

该产品包含在如下化合物库中:
药物功能重定位化合物库 EMA 上市药物库 抑制剂库 NO PAINS 化合物库 免疫/炎症分子化合物库 经典已知活性库 抗病毒库 ReFRAME 相关化合物库 口服活性化合物库 FDA上市及药典收录分子库

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

Ombitasvir 1258226-87-7 Microbiology/Virology Proteases/Proteasome HCV Protease Hepatitis C virus Inhibitor ABT267 奥比他韦 inhibit HCV ABT 267 ABT-267 inhibitor

 

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