Pibrentasvir

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

Pibrentasvir (ABT-530) 是一种新型泛基因型 HCV NS5A 抑制剂，针对含有 NS5A 基因型 1-6 的 HCV 复制子，EC50 为 1.4-5.0 pM。

Pibrentasvir (ABT-530) is a novel and pan-genotypic HCV NS5A inhibitor with EC50 of 1.4-5.0 pM against HCV replicons containing NS5A genotypes 1-6; demonstrates potent antiviral activity and acceptable safety during 3-day monotherapy in patients with HCV genotype 1 infection, with or without compensated cirrhosis.HCV Infection Phase 2 Clinical.

Pibrentasvir inhibits HCV genotype 1a-H77, 1b-Con1, and 2a-JFH-1 subgenomic replicons with 50% effective concentrations (EC50s) of 1.8, 4.3, and 5.0 pM, respectively. The antiviral activity of Pibrentasvir is attenuated 35- to 47-fold in the presence of 40% human plasma through sequestration of compound due to plasma protein binding. Pibrentasvir retains full activity against all of the genotype 1a and 1b single-position NS5A substitutions tested, except Y93H and Y93N in genotype 1a, which confers a ≤7-fold increase in EC50 to Pibrentasvir.

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ABT-530

Microbiology/Virology

HCV

HCVNS5A

Infection

HCV Infection

1353900-92-1

1113.2

C57H65F5N10O8

>98% (HPLC)

DMSO: 60 mg/mL, need ultrasonic （ < 1 mg/ml refers to the product slightly soluble or insoluble )

FC1=CC=C(C2CCN(C3=C(F)C=C(N4[C@@H](C5=C(F)C=C6C(N=C([C@H]7N(C([C@@H](NC(OC)=O)[C@H](OC)C)=O)CCC7)N6)=C5)CC[C@@H]4C8=C(F)C=C9C(N=C([C@H]%10N(C([C@@H](NC(OC)=O)[C@H](OC)C)=O)CCC%10)N9)=C8)C=C3F)CC2)C=C1

Dimethyl ((2S,2'S,3R,3'R)-((2S,2'S)-(((2R,5R)-1-(3,5-difluoro-4-(4-(4-fluorophenyl)piperidin-1-yl)phenyl)pyrrolidine-2,5-diyl)bis(6-fluoro-1H-benzo[d]imidazole-5,2-diyl))bis(pyrrolidine-2,1-diyl))bis(3-methoxy-1-oxobutane-1,2-diyl))dicarbamate

(-20℃)

With Ice Pack

≥ 2 years