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首页 / 抑制剂/激动剂 / 抗感染 / 丙型肝炎病毒 / Dasabuvir/达塞布韦

Dasabuvir/达塞布韦 {[allProObj[0].p_purity_real_show]}

货号：A549431 同义名： 达塞布韦 / ABT-333

Dasabuvir是一种 RNA 依赖性 RNA 聚合酶抑制剂，IC50 范围从 2.2 nM 到 10.7 nM。

Dasabuvir/达塞布韦 化学结构 CAS号：1132935-63-7
Dasabuvir/达塞布韦 化学结构
CAS号：1132935-63-7
Dasabuvir/达塞布韦 3D分子结构
CAS号：1132935-63-7
Dasabuvir/达塞布韦 化学结构 CAS号：1132935-63-7
Dasabuvir/达塞布韦 3D分子结构 CAS号：1132935-63-7
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Dasabuvir/达塞布韦 纯度/质量文件 产品仅供科研

货号：A549431 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

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Dasabuvir/达塞布韦 生物活性

描述 The hepatitis C virus (HCV) is an enveloped, single-strand, positive-sense RNA virus in the Flaviviridae family. The HCV NS5B polymerase has multiple binding sites that can be targeted for inhibition of HCV replication. ABT-333 is a nonnucleoside inhibitor of the RNA-dependent RNA polymerase encoded by the HCV NS5B gene. It inhibited recombinant NS5B polymerases derived from HCV genotype 1a and 1b clinical isolates, with IC50 values between 2.2 and 10.7 nM. In the HCV subgenomic replicon system, dasabuvir inhibited genotype 1a (strain H77) and 1b (strain Con1) replicons with EC50 values of 7.7 and 1.8 nM, respectively. This level of activity was retained against a panel of chimeric subgenomic replicons that contained HCV NS5B genes from 22 genotype 1 clinical isolates from treatment-naive patients, with EC50s ranging between 0.15 and 8.57 nM[3].

Dasabuvir/达塞布韦 细胞实验

Cell Line
Concentration Treated Time Description References
HEK cells (expressing hERG channels) 1-30 µM Concentration-dependently inhibited hERG current with IC50 of 3.2 µM; partially irreversibly blocked channels in the open state. Pharmaceuticals (Basel). 2023 Mar 25;16(4):488.
Canine left ventricular myocardial cells 3-30 µM 5 min Concentration-dependently prolonged APD50 and APD90, elevated early plateau potential, and reduced V+max, VPh1max, and V−max; induced early afterdepolarizations (EADs) in some cells. Pharmaceuticals (Basel). 2023 Mar 25;16(4):488.
Canine left ventricular myocardial cells 1 µM 15 min Prolonged action potential duration (APD90) reversibly by 7.84±3.09%; irreversibly reduced maximal rates of phases 0 and 1 (V+max and VPh1max). Pharmaceuticals (Basel). 2023 Mar 25;16(4):488.
Genotype 1b (Con1 strain) 1.8 nM 3 days Evaluate the inhibitory effect of ABT333 on genotype 1b HCV subgenomic replicons, showing an EC50 of 1.8 nM Antimicrob Agents Chemother. 2015 Mar;59(3):1505-11.
Genotype 1a (H77 strain) 7.7 nM 3 days Evaluate the inhibitory effect of ABT333 on genotype 1a HCV subgenomic replicons, showing an EC50 of 7.7 nM Antimicrob Agents Chemother. 2015 Mar;59(3):1505-11.
Canine Left Ventricular Cells 1.2 µM ABT-333 increases action potential duration and provokes early afterdepolarizations via inhibition of I Kr ABT-333 (Dasabuvir) Increases Action Potential Duration and Provokes Early Afterdepolarizations in Canine Left Ventricular Cells via Inhibition of IKr. Pharmaceuticals 2023, 16, 488.

Dasabuvir/达塞布韦 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
NCT02460133 Hepatitis C Virus Phase 4 Active, not recruiting June 2018 -
NCT03423641 - Completed - -
NCT02057003 - Recruiting December 2020 Spain ... 展开 >> Valme University Hospital Recruiting Seville, Spain, 41014 Contact: Karin Neukam, PhD    0034955015799    karin.neukam@gmail.com    Contact: Juan A Pineda, MD    0034955015684    japineda@telefonica.net 收起 <<

Dasabuvir/达塞布韦 参考文献

[1]Minaei AA, Kowdley KV. ABT-450/ ritonavir and ABT-267 in combination with ABT-333 for the treatment of hepatitis C virus. Expert Opin Pharmacother. 2015 Apr;16(6):929-37.

[2]Asselah T. ABT-450 combined with ritonavir, in addition to ABT-333 and ribavirin: a race for an interferon-free regimen to cure HCV infection. J Hepatol. 2013 Oct;59(4):885-8.

[3]Kati W, Koev G, Irvin M, Beyer J, Liu Y, Krishnan P, Reisch T, Mondal R, Wagner R, Molla A, Maring C, Collins C. In vitro activity and resistance profile of dasabuvir, a nonnucleoside hepatitis C virus polymerase inhibitor. Antimicrob Agents Chemother. 2015 Mar;59(3):1505-11

Dasabuvir/达塞布韦 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.03mL

0.41mL

0.20mL

10.13mL

2.03mL

1.01mL

20.26mL

4.05mL

2.03mL

Dasabuvir/达塞布韦 技术信息

CAS号1132935-63-7
分子式C26H27N3O5S
分子量 493.57
SMILES Code CS(=O)(NC1=CC=C2C=C(C3=CC(N(C(N4)=O)C=CC4=O)=CC(C(C)(C)C)=C3OC)C=CC2=C1)=O
MDL No. MFCD27923655
别名 达塞布韦 ;ABT-333
运输蓝冰
InChI Key NBRBXGKOEOGLOI-UHFFFAOYSA-N
Pubchem ID 56640146
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C
溶解方案

DMSO: 45 mg/mL(91.17 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
方案 三

Tags: Dasabuvir | 1132935-63-7 | ABT-333 | ABT333 | ABT 333 | HCV Polymerase Inhibitor | Anti-infection | Cell Cycle/DNA Damage | HCV | DNA/RNA Synthesis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Dasabuvir/达塞布韦 纯度/质量文件 | Dasabuvir/达塞布韦 生物活性 | Dasabuvir/达塞布韦 临床数据 | Dasabuvir/达塞布韦 参考文献 | Dasabuvir/达塞布韦 实验方案 | Dasabuvir/达塞布韦 技术信息

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