Glecaprevir

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Glecaprevir (ABT 493;A 1282576) 是一种新型 HCV NS3/4A 蛋白酶抑制剂，具有泛基因型活性，在体外抑制 HCV 基因型 1-6 的 NS3/4A 蛋白酶，IC50 为 3.5-11.3 nM。

Glecaprevir (ABT 493;A 1282576) is a novel HCV NS3/4A protease inhibitor with pan-genotypic activity, inhibits NS3/4A proteases from HCV genotypes 1-6 in vitro with IC50 of 3.5-11.3 nM; inhibits the replication of stable HCV subgenomic replicons genotypes 1-6 with EC50 of 0.21-4.6 nM, has a median EC50 of 0.30 nM (0.05 - 3.8 nM) for HCV replicons containing proteases from 40 HCV genotype 1-5 samples; the combination of ABT-493 and ABT-530 demonstrates potent antiviral activity and acceptable safety in clinical trails with HCV genotype 1 infection.HCV Infection Phase 2 Clinical(In Vitro):Glecaprevir inhibits the enzymatic activity of HCV genotype 1-6 NS3/4A proteases with half maximal inhibitory concentration (IC50) values ranging from 3.5 to 11.3 nM in a biochemical assay. Glecaprevir inhibites HCV subgenomic stable replicons containing proteases from HCV genotypes 1a, 1b, 2a, 2b, 3a, 4a, 5a, 6a and 6e in Huh-7 cells with 50% effective concentration (EC50) values ranging from 0.21 to 4.6 nM. Glecaprevir is active against a replicon containing protease from genotype 3, the most difficult-to-treat HCV genotype, with an EC50 value of 1.9 nM, which is 10- and 44-fold lower than those for paritaprevir and grazoprevir, respectively. The median Glecaprevir EC50 values against replicons containing these genotype 1a, 1b, 2a, 2b, 3a, 4a, 4d, and 5a clinical samples are 0.08, 0.29, 1.6, 2.2, 2.3, 0.41, 0.17, and 0.12 nM, respectively, with an overall median EC50 value of 0.30 nM (range=0.05~3.8 nM).

Glecaprevir inhibits the enzymatic activity of HCV genotype 1-6 NS3/4A proteases with half maximal inhibitory concentration (IC50) values ranging from 3.5 to 11.3 nM in a biochemical assay. Glecaprevir inhibites HCV subgenomic stable replicons containing proteases from HCV genotypes 1a, 1b, 2a, 2b, 3a, 4a, 5a, 6a and 6e in Huh-7 cells with 50% effective concentration (EC50) values ranging from 0.21 to 4.6 nM. Glecaprevir is active against a replicon containing protease from genotype 3, the most difficult-to-treat HCV genotype, with an EC50 value of 1.9 nM, which is 10- and 44-fold lower than those for paritaprevir and grazoprevir, respectively. The median Glecaprevir EC50 values against replicons containing these genotype 1a, 1b, 2a, 2b, 3a, 4a, 4d, and 5a clinical samples are 0.08, 0.29, 1.6, 2.2, 2.3, 0.41, 0.17, and 0.12 nM, respectively, with an overall median EC50 value of 0.30 nM (range=0.05~3.8 nM).

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ABT 493 | A 1282576

Microbiology/Virology

HCV

HCVNS3/4Aprotease

Infection

HCV Infection

1365970-03-1

838.87

C38H46F4N6O9S

>98% (HPLC)

DMSO: 80 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

CC1(CC1)S(=O)(=O)NC(=O)C2(CC2C(F)F)NC(=O)C3CC4CN3C(=O)C(NC(=O)OC5CCCC5OCC=CC(C6=NC7=CC=CC=C7N=C6O4)(F)F)C(C)(C)C

(33R,35S,91R,92R,5S,E)-5-(tert-butyl)-N-((1R,2R)-2-(difluoromethyl)-1-(((1-methylcyclopropyl)sulfonyl)carbamoyl)cyclopropyl)-14,14-difluoro-4,7-dioxo-2,8,10-trioxa-6-aza-1(2,3)-quinoxalina-3(3,1)-pyrrolidina-9(1,2)-cyclopentanacyclotetradecaphan-12-ene-35

(-20℃)

With Ice Pack

≥ 2 years