Lufotrelvir

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

Lufotrelvir (PF-07304814) 是 PF-00835231 的磷酸前体，是一种有效的 3CLpro 蛋白酶 (Mpro) 抑制剂，具有 SARS-CoV-2 抗病毒活性。Lufotrelvir 结合并抑制 SARS-CoV-2 3CLpro 活性，Ki 为 174nM。Lufotrelvir 是一种很有前途的单一抗病毒试剂，也可用于与针对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。

Lufotrelvir (PF-07304814), a phosphate proagent of PF-00835231, acts as a potent 3CLpro protease (Mpro) inhibitor with SARS-CoV-2 antiviral activity. Lufotrelvir binds and inhibits SARS-CoV-2 3CLpro activity with a Ki of 174nM. Lufotrelvir 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.

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Once administered through intravenous infusion, Lufotrelvir is cleaved into PF-00835231 to exert its anti-viral effects. Lufotrelvir exhibits a favorable cardiovascular safety profile.Lufotrelvir 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.

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Others

Other Targets

SARS-CoV

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2468015-78-1

552.51

C24H33N4O9P

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 130 mg/mL (235.29 mM; 超声助溶 ) H2O 中的溶解度 : 50 mg/mL (90.50 mM; 超声助溶)

O(C)C1=C2C(NC(C(N[C@H](C(N[C@@H](C[C@H]3C(=O)NCC3)C(COP(=O)(O)O)=O)=O)CC(C)C)=O)=C2)=CC=C1

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(-20℃)

With Ice Pack

≥ 2 years