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|
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.
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.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.