PF-07321332 (Nirmatrelvir, Paxlovid) | SARS-CoV-2 Mpro inhibitor

Chemical Structure : PF-07321332

CAS No.: 2628280-40-8

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PF-07321332 (Nirmatrelvir, Paxlovid, PF07321332)

货号: PC-72607Not For Human Use, Lab Use Only.

PF-07321332 (Nirmatrelvir, Paxlovid) is the first, orally bioavailable SARS-CoV-2 main protease (Mpro) inhibitor with biochemical Ki of 3.11 nM.

规格	价格	库存
5 mg	￥1180	In stock
10 mg	￥1780	In stock
25 mg	￥2980	In stock
50 mg	￥4880	In stock
100 mg		Get quote

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生物&药学活性

PF-07321332 (Nirmatrelvir, Paxlovid) is the first, orally bioavailable SARS-CoV-2 main protease (Mpro) inhibitor with biochemical Ki of 3.11 nM.
PF-07321332 demonstrated highly potent Vero E6 antiviral activity (EC50=74.5 nM).
PF-07321332 inhibited SARS-CoV-2-induced CPE in Vero E6 cells enriched for ACE2 with EC50 of 4.48 uM.
PF-07321332 demonstrated potent inhibition in FRET Mpro assays representing Mpro from all coronavirus types known to infect humans, including beta-coronaviruses (SARS-CoV-2, SARS-CoV-1, HKU1, OC43, and MERS-CoV) as well as alpha-coronaviruses (229E and NL63).
PF-07321332 inhibited SARS-CoV-2 replication as assessed using a nanoluciferase reporter virus in A549-ACE2 cells with EC50 and EC90 values of 77.9 and 215 nM, respectively, with no cytotoxicity.
PF-07321332 demonstrated potent antiviral activity against SARS-CoV-1 (EC90=317 nM), MERS-CoV (EC90=351 nM), and 229E (EC90=620 nM) in CPE assays.
PF-07321332 demonstrated in vivo efficacy against SARS-CoV-2 MA10 infection in mouse-adapted SARS-CoV-2 model.
PF-07321332 demonstrated a favorable off-target selectivity profile in a broad panel of G protein–coupled receptors, kinases, transporters, and phosphodiesterase enzyme inhibitor screens, and was devoid of activity against the cardiac ion channels Kv1.1, Cav1.2, and Nav1.5, and was not mutagenic or clastogenic in in vitro genetic toxicity studies.

物理化学性质&存储条件

分子量	499.535
分子式	C23H32F3N5O4
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	(1R,2S,5S)-N-((S)-1-cyano-2-((S)-2-oxopyrrolidin-3-yl)ethyl)-3-((S)-3,3-dimethyl-2-(2,2,2-trifluoroacetamido)butanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide

参考文献

1. Pavan M, et al. J Enzyme Inhib Med Chem. 2021 Dec;36(1):1646-1650.

2. Owen DR, et al. Science. 2021 Dec 24;374(6575):1586-1593.

3. Alugubelli YR, et al. bioRxiv. 2021 Dec 21:2021.12.18.473330.

4. Abe K, et al. Sci Rep. 2022 Jan 25;12(1):1299.

PF-07321332 (Nirmatrelvir, Paxlovid, PF07321332)

生物&药学活性

物理化学性质&存储条件

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PF-07321332 (Nirmatrelvir, Paxlovid, PF07321332)

生物&药学活性

物理化学性质&存储条件

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