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MK-3207 hydrochloride is a potent and orally bioavailable calcitonin gene-related peptide (CGRP) receptor antagonist. MK-3207 potently inhibits human α-CGRP-induced cAMP production in HEK293 cells stably expressing human CLR/RAMP1 with an IC50 of 0.12 nM, and maintains similar potency in the presence of 50% human serum with an IC50 of 0.17 nM, indicating that the activity of MK-3207 would not be dramatically affected by plasma protein binding in vivo. MK-3207 displays lower affinity for CGRP receptors from other species, including canine and rodent. MK-3207 produced a concentration-dependent inhibition of dermal vasodilation, with plasma concentrations of 0.8 and 7 nM required to block 50 and 90% of the blood flow increase, respectively. In vitro, MK-3207 is a potent antagonist of the human and rhesus monkey CGRP receptors (K(i) = 0.024 nM).
| Molecular Weight | 594.05 |
| Formula | C31H29F2N5O3.HCl |
| CAS Number | 957116-20-0 |
| Solubility (25°C) | DMSO 110 mg/mL Ethanol 110 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related CGRP Receptor Products |
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| 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 |
| MK-0974
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. |
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| 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. |
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