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).
| Molecular Weight | 594.05 |
| Formula | C31H29F2N5O3.HCl |
| CAS Number | 957116-20-0 |
| Solubility (25°C) | DMSO 110 mg/mL Ethanol 110 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
| Related CGRP Receptor Products |
|---|
| Adrenomedullin (16-31), human
Adrenomedullin (16-31), human is amino acid residues 16-31 fragment of human adrenomedullin (hADM). |
| α-CGRP(human)
α-CGRP(human) is a regulatory neuropeptide of 37 amino acids. |
| Adrenomedullin (AM) (22-52), human
Adrenomedullin (AM) (22-52), human is an adrenomedullin receptor antagonist, and also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat. |
| Calcitonin Gene Related Peptide (CGRP) II, rat
Calcitonin Gene Related Peptide (CGRP) II, rat, a CGRP receptor activator, is a potent and long-lasting vasodilator. |
| Adrenomedullin (11-50), rat
Adrenomedullin (11-50), rat is the C-terminal fragment (11-50) of rat adrenomedullin. |
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