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Product introduction
PF-07321332是SARS-CoV-2 main protease (Mpro,也称为3CL蛋白酶)的可逆共价抑制剂,ki为3.11 nM。PF- 07321332 直接与酶的催化半胱氨酸 (Cys145) 残基结合。 PF-07321332是一种抗病毒药物,是3CL蛋白酶抑制剂。它是一种共价抑制剂,可直接与蛋白酶的半胱氨酸催化残基(Cys145)结合。该药与利托那韦的复方制剂,以PAXLOVID为商品名,用于联合治疗COVID-19的3期临床试验正在进行中。在这一治疗组合中,利托那韦的作用是减缓细胞色素酶对PF-07321332的代谢,以维持更高的主药循环浓度。冠状病毒蛋白酶会在病毒多聚蛋白的多处位置进行裂解,裂解的位置通常位于谷氨酸残基之后。有关人类鼻病毒的早期研究显示,灵活的谷氨酸侧链可被刚性的吡咯烷酮取代。随后,这类药物被进一步开发用于治疗包括SARS在内的其他疾病。当GC376(GC373的前体药物)被用来治疗曾经100%致死的猫冠状病毒病,即由FIPV引发的猫传染性腹膜炎时,靶向3CL蛋白酶的效用首次在现实世界中得到了证明。此产品正是GC373的类似物,其中的醛共价半胱氨酸受体被腈所取代。PF-07321332是通过修改前期临床候选药物PF-07304814而开发的。PF-07304814也是一种共价抑制剂,但其弹头(warhead)是一种羟基酮的磷酸盐前药。PF-07304814需要静脉注射,这限制了它只能在医院使用。
Chinese name
PF-07321332
English name
PF-07321332
Chinese alias
-
English alias
BDBM496902 | 2628280-40-8 | (1R,2S,5S)-N-{(1S)-1-cyano-2-[(3S)-2-oxopyrrolidin-3-yl]ethyl}-6,6-dimethyl-3-[3-methyl-N-(trifluoroacetyl)-L-valyl]-3-azabicyclo[3.1.0]hexane-2-carboxamide | SCHEMBL24108848 | (1R,2S,5S)-N-[(1S)-1-cyano-2-[(3S)-2-oxopyrrolidin
CAS number
2628280-40-8
molecular formula
C23H32F3N5O4
molecular weight
499.53 g/mol
Exact mass
-
PSA
131.000 Ų
Logp
2.2
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Research chemical CAS 2628280-40-8 98% 1g

Yuanye Research chemical CAS 2628280-40-8 98% 1g, complete specifications; suitable for production, research, laboratory testing and inspection; digital one-stop procurement platform for scientific materials.

item number:S33327-1g
Product model:1g
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