PeptideDB

MK-3207

CAS: 957118-49-9 F: C31H29F2N5O3 W: 557.59

MK-3207 is an orally active, highly selective and species-specific CGRP receptor antagonist (for human CGRP receptor: IC
Data collection:peptidedb@qq.com

This product is for research use only, not for human use. We do not sell to patients.

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.