| Bioactivity | MK-3207 is an orally active, highly selective and species-specific CGRP receptor antagonist (for human CGRP receptor: IC50=0.12 nM; Ki=0.024 nM). MK-3207 can be used for migraine studies[1]. |
| Invitro | MK-3207 (0.3, 0.6, 1.1, 2.3, 4.5, 9.0 nM; 30 min) potently blocks human α-CGRP-stimulated cAMP responses in human CGRP receptor-expressing HEK293 cells[1]. Cell Viability Assay[1] Cell Line: |
| In Vivo | MK-3207 (0.3, 0.6, 2.1, 9.1, 21.2, 60.6 µg/kg; i.v.; single) inhibits CIDV in rhesus monkeys with EC50 and Emax values of approximately 0.8 nM and 81%[1].MK-3207 (10 mg/kg; p.o.; single) shows the CSF/plasma ratio is 2 to 3%[1]. Animal Model: |
| Name | MK-3207 |
| CAS | 957118-49-9 |
| Formula | C31H29F2N5O3 |
| Molar Mass | 557.59 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| Reference | [1]. Salvatore CA, Moore EL, Calamari A, Pharmacological properties of MK-3207, a potent and orally active calcitonin gene-related peptide receptor antagonist. J Pharmacol Exp Ther. 2010 Apr;333(1):152-60. |