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MK-0974 is an orally bioavailable antagonist of the calcitonin gene-related peptide (CGRP) receptor complex (Ki = 0.77 ?M), which is composed of the calcitonin receptor-like receptor (CRLR) and receptor activity modifying protein 1 (RAMP1).{38703} MK-0974 binds selectively to the human CGRP receptor complex, over the adrenomedullin receptor complexes, which are composed of CRLR and RAMP2 or RAMP3 (Kis = >100 and 29 ?M, respectively, in HEK293 cells). MK-0974 also binds to rhesus, canine, and rat CGRP receptor complexes (Kis = 1.2, 1,204, and 1,192 nM, respectively). MK-0974 inhibits cAMP accumulation stimulated by CGRP (Item No. 24405) with an IC50 value of 2.2 nM in HEK293 cells expressing the CGRP receptor complex. Ex vivo, MK-0974 (5 ?M) reduces CGRP-induced vasodilation in isolated human meningeal arteries.{38704} MK-0974 also inhibits vasodilation induced by topical application of capsaicin (Item No. 92350) in rhesus monkeys (EC50 = 127 nM).{38703}
Territorial Availability: Available through Bertin Technologies only in France
| Size | 1 mg, 10 mg, 5 mg |
|---|---|
| Shipping | dry ice |
| CAS number | 781649-09-0 |
| Molecular formula | C26H27F5N6O3 |
| Smiles | O=C(N[C@@H]1CC[C@@H](C2=CC=CC(F)=C2F)CN(CC(F)(F)F)C1=O)N3CCC(N4C(NC5=C4C=CC=N5)=O)CC3 |
| Molecular weight | 566,5 |
| Custom code | 2933.39 |
| Formulation | A crystalline solid |
| Purity | ≥98% |
| 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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