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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 |
|---|
| MK-3207 hydrochloride
MK-3207 hydrochloride is a potent CGRP receptor antagonist with IC50 of 0.12 nM. |
| Rimegepant
Rimegepant, also known as BMS-927711, is a potent, selective, competitive, and orally active calcitonin gene-related peptide (CGRP) antagonist with a Ki value of 0.027 nM. |
| BAR 501 impurity |
| BAR501
BAR501 is a potent and selective agonist of GPBAR1 with an EC50 of 1 μM. |
| Olcegepant (BIBN-4096)
Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide (CGRP) receptor with IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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