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PF-07321332 is an orally bioavailable inhibitor of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (Mpro), also known as 3C-like protease (3CLpro), with a Ki value of 3.11 nM.{62563} It also inhibits Mpro from other members of the Betacoronavirus genus, including SARS-CoV-1, HKU1-CoV, OC43-CoV, and MERS-CoV (Kis = 4.94, 189, 36.4, and 187 nM, respectively), as well as Mpro from NL-63-CoV and 229E CoV (Kis = 226 and 44.4 nM, respectively), which are members of the Alphacoronavirus genus. PF-07321332 is selective for these enzymes over several other proteases, including human and HIV-1 proteases (IC50s = >100 µM for all), as well as a panel of G protein-coupled receptors, kinases, and transporters (IC50s = ?100 µM for all). It inhibits SARS-CoV-2 replication in A549 cells (EC50 = 77.9 nM) and reduces the cytopathic effect of SARS-CoV-2 in infected Vero E6 cells (EC50 = 74.5 nM) with a 50% cytotoxic concentration (CC50) value of greater than 100 µM. PF-07321332 (300 and 1,000 mg/kg) reduces lung viral titers and the severity of pulmonary lesions in mice infected with the mouse-adapted SARS-CoV-2 MA10 variant. Formulations containing PF-07321332 have been used in the treatment of COVID-19.
Territorial Availability: Available through Bertin Technologies only in France
| Size | 1 mg, 10 mg, 25 mg, 5 mg |
|---|---|
| Shipping | dry ice |
| CAS number | 2628280-40-8 |
| Molecular formula | C23H32F3N5O4 |
| Smiles | FC(F)(F)C(N[C@@H](C(C)(C)C)C(N1C[C@@](C2(C)C)([H])[C@@]2([H])[C@H]1C(N[C@H](C#N)C[C@H]3C(NCC3)=O)=O)=O)=O |
| Molecular weight | 499,5 |
| Custom code | 2933.79 |
| Formulation | A solid |
| Purity | ≥95% |
| UNSPSC code | 12352100 |
Cayman Chemical’s mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.
Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.
Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.
Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.
Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009
Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.
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