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Telcagepant Telcagepant is a calcitonin gene-related peptide(CGRP) receptor antagonist under development for the acute treatment and prevention of migraine. It is a highly potent, selective, and orally bioavailable antagonist of the human (K(I) = 0.77 nM) and rhesus (K(I) = 1.2 nM) CGRP receptors, which displays 1500-fold lower affinity for the canine and rat receptors as determined via (125)I-human CGRP competition binding assays in vitro. It displayed moderate clearance (14-20 ml min(-1) kg(-1)) in monkeys, while oral bioavailability was 6%. It was developed by Merck & Co. It was found to have equal potency to rizatriptan and zolmitriptan in two Phase III clinical trials in the acute treatment of migraine. But the company has now terminated development of the drug. Uses: Telcagepant is used to acute treatment and prevention of migraine. Synonyms: MK 0974; MK0974; MK-0974; N-[(3R,6S)-6-(2,3-Difluorophenyl)hexahydro-2-oxo-1-(2,2,2-trifluoroethyl)-1H-azepin-3-yl]-4-(2,3-dihydro-2-oxo-1H-imidazo[4,5-b]pyridin-1-yl)-1-piperidinecarboxamide;N-(6-(2,3-Difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl)-4-(2-oxo-2,3-dihydro-1H-imidazo(4,5-B)pyridin-1-yl)piperidine-1-carboxamide. Grades: 95%. CAS No. 781649-09-0. Molecular formula: C26H27F5N6O3. Mole weight: 566.53. BOC Sciences 11
Telcagepant Telcagepant (MK-0974) is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist with K i s of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively. Uses: Scientific research. Group: Signaling pathways. Alternative Names: MK-0974. CAS No. 781649-09-0. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-32709. MedChemExpress MCE
1,3-Dihydro-1-(4-piperidinyl)-2H-imidazo[4,5-b]pyridin-2-one Dihydrochloride 1,3-Dihydro-1-(4-piperidinyl)-2H-imidazo[4,5-b]pyridin-2-one is an intermediate used to prepare (3R,6S)-3-amino-6-(2,3-difluorophenyl)azepan-2-one of Telcagepant (MK-0974) for use as a calcitonin gene-related peptide receptor antagonist treating migraine headaches. Group: Biochemicals. Grades: Highly Purified. CAS No. 781649-84-1. Pack Sizes: 100mg, 500mg. Molecular Formula: C11H16Cl2N4O. US Biological Life Sciences. USBiological 9
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