Dasabuvir

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Chemical Structure| 1132935-63-7 同义名 : 达塞布韦 ;ABT-333
CAS号 : 1132935-63-7
货号 : A549431
分子式 : C26H27N3O5S
纯度 : 99%+
分子量 : 493.575
MDL号 : MFCD27923655
存储条件:

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

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

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

动物实验配方:
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].
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 <<
实验方案
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

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