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Avacopan is an antagonist of the complement 5a1 (C5a1) receptor (IC50 = 0.1 nM).{64646} It is selective for C5a1 over the C5a2 receptor and chemokine-like receptor 2 (CMKLR2), also known as chemerin receptor 2 or GPR1 (IC50s = >10,000 nM for both), as well as the C3a receptor, CMKLR1, and formyl peptide receptor 1 (FPR1; IC50s = >10,000 nM for all), and over panels of 18 chemokine receptors (IC50s = ?6,700 nM for all), 54 other receptors at 10 µM, and five cytochrome P450 (CYP) isoforms (IC50s = >10,000 nM for all). Avacopan (50 nM) reduces the migration of isolated cynomolgus monkey neutrophils. It also reduces C5a-induced increases in neutrophil cell surface levels of CD11b in whole blood isolated from mice with a knock-in of human C5AR1, the gene encoding the C5a1 receptor, when used at concentrations of 10 and 100 nM or when administered at doses of 0.075 or 0.15 mg/kg. Formulations containing avacopan have been used in the adjunctive treatment of severe vasculitis associated with anti-neutrophil cytoplasmic autoantibodies (ANCA).
Territorial Availability: Available through Bertin Technologies only in France
| Size | 1 mg, 10 mg, 25 mg, 5 mg |
|---|---|
| Shipping | dry ice |
| CAS number | 1346623-17-3 |
| Molecular formula | C33H35F4N3O2 |
| Smiles | O=C(C1=C(C=CC=C1F)C)N2[C@](C3=CC=C(C=C3)NC4CCCC4)([H])[C@H](CCC2)C(NC5=CC(C(F)(F)F)=C(C=C5)C)=O |
| Molecular weight | 581,6 |
| Custom code | 2933.39 |
| Formulation | A solid |
| Purity | ≥95% (mixture of isomers) |
| 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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