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MK-0974 (Telcagepant) is a highly potent, selective, and orally bioavailable CGRP receptor antagonist with Ki values of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors respectively. MK-0974 displays >1500-fold lower affinity for the canine and rat receptors. MK-0974 displays reversible and saturable binding to both SK-N-MC membranes and rhesus cerebellum with a K(D) of 1.9 nM and 1.3 nM, respectively.
| Molecular Weight | 566.52 |
| Formula | C26H27F5N6O3 |
| CAS Number | 781649-09-0 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related CGRP Receptor Products |
|---|
| Adrenomedullin (16-31), human
Adrenomedullin (16-31), human is amino acid residues 16-31 fragment of human adrenomedullin (hADM). |
| α-CGRP(human)
α-CGRP(human) is a regulatory neuropeptide of 37 amino acids. |
| Adrenomedullin (AM) (22-52), human
Adrenomedullin (AM) (22-52), human is an adrenomedullin receptor antagonist, and also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat. |
| Calcitonin Gene Related Peptide (CGRP) II, rat
Calcitonin Gene Related Peptide (CGRP) II, rat, a CGRP receptor activator, is a potent and long-lasting vasodilator. |
| Adrenomedullin (11-50), rat
Adrenomedullin (11-50), rat is the C-terminal fragment (11-50) of rat adrenomedullin. |
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Products are for research use only. Not for human use. We do not sell to patients.
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