PF-07304814 是 PF-00835231 的磷酸前药，是一种有效的 3CLpro 蛋白酶 (Mpro) 抑制剂，具有 SARS-CoV-2 抗病毒活性。PF-07304814 结合并抑制 SARS-CoV-2 3CLpro 活性，Ki 为 174nM。PF-07304814 是一种很有前途的单一抗病毒试剂，也可用于与针对冠状病毒生命周期其他关键阶段的其他抗病毒试剂的联合研究。
货号:ajcx34228
CAS:2468015-78-1
分子式:C24H33N4O9P
分子量：552.51
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PF-07304814, a phosphate prodrug of PF-00835231, acts as a potent 3CLpro protease (Mpro) inhibitor with SARS-CoV-2 antiviral activity. PF-07304814 binds and inhibits SARS-CoV-2 3CLpro activity with a Ki of 174nM. PF-07304814 is promising single antiviral agent and also can be used for the research of combination with other antivirals that target other critical stages of the coronavirus life cycle[1].

Once administered through intravenous infusion, PF-07304814 is cleaved into PF-00835231 to exert its anti-viral effects. PF-07304814 exhibits a favorable cardiovascular safety profile[1].PF-07304814 is administered intravenously to rats, dogs and monkeys. It exhibits high systemic clearance and short half-life across species forming 68, 81, 76% PF-00835231 in rats, dogs and monkey respectively in comparison to the systemic exposure achieved with IV administration of PF00835231[1].

[1]. Koen Vandyck, et al. Considerations for the discovery and development of 3-chymotrypsin-like cysteine protease inhibitors targeting SARS-CoV-2 infection. Curr Opin Virol. 2021 Apr 27;49:36-40.
[2]. Britton Boras, et al. Title: Discovery of a Novel Inhibitor of Coronavirus 3CL Protease as a Clinical Candidate for the Potential Treatment of COVID-19 Short Title: Novel 3CL Protease Inhibitor for COVID-19