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首页-小分子抑制剂&激动剂-Antibiotics and Antivirals-HBV-GS-8873
GS-8873

Chemical Structure : GS-8873

CAS No.: 2241575-59-5

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GS-8873 (GS8873)

货号: PC-22186Not For Human Use, Lab Use Only.

GS-8873 is a potent, orally bioavailable inhibitor of HBV surface antigen (HBsAg) with EC50 of 4 nM in HepG2-NTCP assays, via inhibition of the human poly(A) polymerases PAPD5/7, promoting destabilization and degradation of HBV mRNA.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

GS-8873 is a potent, orally bioavailable inhibitor of HBV surface antigen (HBsAg) with EC50 of 4 nM in HepG2-NTCP assays, via inhibition of the human poly(A) polymerases PAPD5/7, promoting destabilization and degradation of HBV mRNA.
GS-8873 exhibits excellent cellular activity and preclinical pharmacokinetic parameters superior to RG7834.
GS-8873 was shown to cause neuroelectrophysiology deficits in rats and monkeys, leading to its discontinuation.

物理化学性质&存储条件

分子量 442.51
分子式 C24H30N2O6
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(R)-11-(methoxymethyl)-12-(3-methoxypropoxy)-3,3-dimethyl-8-oxo-2,3,8,13b-tetrahydro-1H-pyrido[2,1-a]pyrrolo[1,2-c]phthalazine-7-carboxylic acid

参考文献

1. Kato D, et al. ACS Med Chem Lett. 2024 Mar 22;15(4):546-554.

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