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.
|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.
Examining the binding properties of MK-0974: a CGRP receptor antagonist for the acute treatment of migraine.
Moore EL, et al. Eur J Pharmacol. 2009 Jan 14;602(2-3):250-4. PMID: 19084002.
|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-3207 hydrochloride is a potent CGRP receptor antagonist with IC50 of 0.12 nM.
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