Glecaprevir

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Chemical Structure| 1365970-03-1 同义名 : ABT-493;A-1282576
CAS号 : 1365970-03-1
货号 : A471517
分子式 : C38H46F4N6O9S
纯度 : 99%+
分子量 : 838.865
MDL号 : MFCD30533436
存储条件:

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 85 mg/mL(101.33 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 Hepatitis C virus (HCV) is an enveloped, single-stranded, positive-sense RNA virus in the Flaviviridae family. The serine protease encoded by the HCV NS3 and NS4A genes is an attractive target for the discovery of direct-acting antivirals (DAAs). Glecaprevir is a novel HCV NS3/4A protease inhibitor (PI) with pangenotypic activity. It inhibited the enzymatic activity of purified NS3/4A proteases from HCV genotypes 1 to 6 in vitro (IC50 = 3.5 to 11.3 nM) and the replication of stable HCV subgenomic replicons containing proteases from genotypes 1 to 6 (EC50 = 0.21 to 4.6 nM). Glecaprevir had a median EC50 of 0.30 nM (range, 0.05 to 3.8 nM) for HCV replicons containing proteases from 40 samples from patients infected with HCV genotypes 1 to 5. Of note, glecaprevir was active against a replicon containing the protease from genotype 3, the most-difficult-to-treat HCV genotype, with an EC50 of 1.9 nM[3]. Genotype 3-infected patients who were treated for 12 weeks had a rate of sustained virologic response at 12 weeks of 95% (95% CI, 93 to 98; 222 of 233 patients) with once-daily glecaprevir-pibrentasvir (a direct-acting antiviral agent)[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.19mL

0.24mL

0.12mL

5.96mL

1.19mL

0.60mL

11.92mL

2.38mL

1.19mL

参考文献

[1]Lin CW, Dutta S, et al. Pharmacokinetics, Safety, and Tolerability of Single and Multiple Doses of ABT-493: A First-In-Human Study. J Pharm Sci. 2017 Feb;106(2):645-651.

[2]Gane E, Poordad F, et al. High Efficacy of ABT-493 and ABT-530 Treatment in Patients With HCV Genotype 1 or 3 Infection and Compensated Cirrhosis. Gastroenterology. 2016 Oct;151(4):651-659.e1.

[3]Ng TI, Tripathi R, Reisch T, et al. In Vitro Antiviral Activity and Resistance Profile of the Next-Generation Hepatitis C Virus NS3/4A Protease Inhibitor Glecaprevir. Antimicrob Agents Chemother. 2017;62(1):e01620-17

[4]Zeuzem S, Foster GR, Wang S, et al. Glecaprevir-Pibrentasvir for 8 or 12 Weeks in HCV Genotype 1 or 3 Infection. N Engl J Med. 2018;378(4):354‐369