GSK-2485852

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

GSK-2485852 (GSK2485852, GSK5852) 是一种高效、选择性 HCV NS5B 聚合酶抑制剂，在复制子测定中对 HCV 基因型 1a 和 1b 的 IC50 分别为 3.0 和 1.6 nM。

GSK-2485852 (GSK2485852, GSK5852)?is a highly potent, selective HCV NS5B polymerase inhibitor with IC50 of 3.0 and 1.6 nM for HCV genotypes 1a and 1b in replicon assay, respectively; displays an excellent resistance profile and shows a <5-fold potency loss across the clinically important NS5B resistance mutations P495L, M423T, C316Y, and Y448H; targets NNI palm site 2 of NS5B and inhibits all HCV genotypes.HCV Infection Phase 1 Clinical.

Nonstructural protein 5B (NS5B) RNA-dependent RNA polymerase (RdRp) is a component of HCV, for researching HCV infection-related diseases.GSK5852 (compound 87) inhibits aggregation by two mechanisms: 1) stabilizing β-flap in a closed inactive state to inhibit the initiation step of the RdRp RNA replication cycle; 2) disruption of RNA processing channels through direct spatial contact.GSK5852 is a non-nucleoside NS5B inhibitor and exhibits inhibitory effect on HCV mutant variants with EC50s of 3.2 nM (GT1a C316Y), 1.9 nM (GT1b C316N), respectively.GSK5852 displays an excellent resistance profile and shows a <5-fold potency loss across the clinically important NS5B resistance mutations.GSK5852 shows no cross-resistance against known resistance mutations in NS5B.GSK5852 (compound 3) (0-10 μM) blocks the initiation step of NS5B polymerase cycle.GSK5852 (0.6, 10 μM; 0-75 h) shows slow binding kinetics with isolated GT1b 316N protein, and with a dissociation half-life of >40 hours.GSK5852 (0.6, 10 μM; 15 min) inhibits NS5B?21 1b 316N with an IC50 value of 130 nM.Western Blot Analysis Cell Line:HCV NS5B Concentration:0, 0.016, 0.08, 0.4, 2, 10 μM Incubation Time:Result:Resulted migration of CTP substrate (at 10 μM), decreased pCpG reaction product with increasing concentrations and significantly decreased at a dosage >2 μM.

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GSK2485852 | GSK 2485852 | GSK-5852

Microbiology/Virology

HCV

HCV

Infection

HCV Infection

1331942-30-3

554.3718

C27H25BF2N2O6S

>98% (HPLC)

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OB(C1=CC=C(CN(C2=C(C3CC3)C=C4C(C(NC)=O)=C(C5=CC=C(F)C=C5)OC4=C2)S(=O)(C)=O)C=C1F)O

B-[4-[[[5-Cyclopropyl-2-(4-fluorophenyl)-3-[(methylamino)carbonyl]-6-benzofuranyl](methylsulfonyl)amino]methyl]-2-fluorophenyl]boronic acid

(-20℃)

With Ice Pack

≥ 2 years