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MK-3207

CAT: 0931-T21558-01Size: 25 mgDry Ice: NoHazardous: No
CAT#:0931-T21558-01Size:25 mg
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AVAILABILITY
24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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CAS Number
957118-49-9
Target
CGRP Receptor
Related Pathways
Neuroscience|||GPCR/G Protein
Bioactivity
MK-3207 is a highly potent and orally bioavailable small molecule antagonist of the calcitonin gene-related peptide (CGRP) receptor, demonstrating an in vitro IC50 of 0.12 nM and a Ki of 0.024 nM for the human receptor with exceptional selectivity over the related human AM1, AM2, CTR, and AMY3 receptors, though it exhibits lower affinity for CGRP receptors from other species such as canine and rodent; in vitro studies confirm its potent antagonism of human and rhesus monkey CGRP receptors (K (i) = 0.024 nM), and in vivo models show it produces a concentration-dependent inhibition of dermal vasodilation, requiring plasma concentrations of 0.8 nM and 7 nM to block 50% and 90% of the blood flow increase, respectively.
Smiles
O=C1[C@@]2(C=3C(N1)=NC=CC3)CC=4C(C2)=CC=C(NC(CN5[C@@H](CNC6(C5=O)CCCC6)C7=CC(F)=CC(F)=C7)=O)C4
Molecular Formula
C31H29F2N5O3
Molecular Weight
557.59
Shipping Conditions
Cool pack
Storage Temperature
-20°C

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