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).
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 110 mg/mL
Ethanol 110 mg/mL
Randomized controlled trial of the CGRP receptor antagonist MK-3207 in the acute treatment of migraine.
Hewitt DJ, et al. Cephalalgia. 2011 Apr;31(6):712-22. PMID: 21383045.
Pharmacological properties of MK-3207, a potent and orally active calcitonin gene-related peptide receptor antagonist.
Salvatore CA, et al. J Pharmacol Exp Ther. 2010 Apr;333(1):152-60. PMID: 20065019.
|Related CGRP Receptor Products|
BAR501 is a potent and selective agonist of GPBAR1 with an EC50 of 1 μM.
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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