MK-3207 HCl 957116-20-0

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Molecular Weight:

594.05 MK-3207 is a Potent CGRP Receptor Antagonist with IC50 and Kiof 0.12 nM and 0.022 nM, highly selective versus human AM1, AM2, CTR, and AMY3. Phase 2.

Biological Activity

MK 3207 exhibits significantly higher affinity for both native and
recombinant human CGRP receptor, as well as rhesus monkey CGRP receptor
with Ki of 24 pM, ~24 pM and 22 pM, respectively, as compared to CGRP receptors from other species, including canine and rodent (Ki values of ~10 nM).


Although has affinity for AMY1 (CTR/RAMP1) receptor with a Ki value of 0.75 nM, MK 3207 displays marked selectivity for human CGRP receptor versus related human AM1 (CLR/RAMP2) receptor, AM2 (CLR/RAMP3) receptor, AMY3 (CTR/RAMP3) receptor, and CTR with Ki values of 16.5 μM, 0.156 μM, 0.128 μM and 1.9 μM, respectively.


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 exhibits
approximately 65-fold more potent in the human serum-shifted in vitro
functional assay than telcagepant with an IC50 of 10.9 nM.


Administration of MK 3207 produces a concentration-dependent inhibition
of capsaicin-induced dermal vasodilation in rhesus monkeys, blocking the
blood flow increase with an EC50 of 0.8 nM and an EC90 of 7 nM,
respectively. MK 3207 displays approximately 100-fold more potent in the
rhesus monkey CIDV assay versus telcagepant with an EC90 of 994 nM.

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Product Categories : GPCR & G Protein > CGRP Receptor Inhibitor