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首页-新冠病毒相关-SARS-CoV-2 Inhibitors-PF-07817883
PF-07817883

Chemical Structure : PF-07817883

CAS No.: 2755812-39-4

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PF-07817883 (Ibuzatrelvir, PF07817883)

货号: PC-22258Not For Human Use, Lab Use Only.

PF-07817883 (Ibuzatrelvir) is a second-generation, orally bioavailable, SARS-CoV-2 main protease (Mpro) with Ki value of 2.48 nM, EC50 of 180 nM for inhibition of SARS-CoV-2 induced cytopathic effect (CPE).

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1 mg ￥1880 In stock
5 mg ￥4580 In stock
10 mg ￥7580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PF-07817883 (Ibuzatrelvir) is a second-generation, orally bioavailable, SARS-CoV-2 main protease (Mpro) with Ki value of 2.48 nM, EC50 of 180 nM for inhibition of SARS-CoV-2 induced cytopathic effect (CPE).
PF-07817883 (Ibuzatrelvir) shows improved metabolic stability versus nirmatrelvir, the antiviral component of the ritonavir-boosted therapy Paxlovid.
PF-07817883 (Ibuzatrelvir) inhibits the SARS-CoV-1 Mpro (IC50 = 18 nM) and MERS Mpro (IC50 = 930 nM) activity, respectively, but has a much smaller disparity in the cell-based antiviral assays (SARS-CoV-1 EC50 = 157 nM and MERS EC50 = 158 nM).
PF-07817883 (Ibuzatrelvir) potently inhibits SARS-CoV-2 viral replication with EC50 and EC90 values of 34 nM and 70 nM respectively in Vero76 cells.
PF-07817883 (Ibuzatrelvir) also demonstrated oral efficacy in a mouse-adapted SARS-CoV-2 model at plasma concentrations equivalent to nirmatrelvir.

物理化学性质&存储条件

分子量 489.50
分子式 C21H30F3N5O5
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

methyl ((S)-1-((2S,4R)-2-(((S)-1-cyano-2-((S)-2-oxopyrrolidin-3-yl)ethyl)carbamoyl)-4-(trifluoromethyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)carbamate

参考文献

1. Allerton CMN, et al. J Med Chem. 2024 Apr 30. doi: 10.1021/acs.jmedchem.3c02469.

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