MK-3207

• CAT Number: I008059
• CAS Number: 957118-49-9
• Molecular Formula: C31H29F2N5O3
• Molecular Weight: 557.59
• Purity: ≥95%
• Target: CGRP
• Solubility: Soluble in DMSO, not in water
• Storage: Store at -20°C
• InChI: InChI=1S/C31H29F2N5O3/c32-21-10-19(11-22(33)13-21)25-16-35-31(7-1-2-8-31)29(41)38(25)17-26(39)36-23-6-5-18-14-30(15-20(18)12-23)24-4-3-9-34-27(24)37-28(30)40/h3-6,9-13,25,35H,1-2,7-8,14-17H2,(H,36,39)(H,34,37,40)
• InChIKey: AZAANWYREOQRFB-UHFFFAOYSA-N
• SMILES: O=C(NC1=CC2=C(CC3(C4=CC=CN=C4NC3=O)C2)C=C1)CN(C5=O)C(C6=CC(F)=CC(F)=C6)CNC75CCCC7

MK-3207 (CAT: I008059) is a potent and orally active calcitonin gene-related peptide (CGRP) receptor antagonist. It acts by binding to the CGRP receptor with high affinity (Ki = 0.024 nM), effectively blocking the interaction of CGRP with its receptor. CGRP is a neuropeptide involved in the pathophysiology of migraine, and CGRP receptor antagonists have shown efficacy in the acute treatment of migraines. MK-3207 has the potential to provide relief from migraine symptoms by inhibiting CGRP signaling and reducing the associated neurogenic inflammation.

Reference

1:Characterizing the PK/PD relationship for inhibition of capsaicin-induced dermal vasodilatation by MK-3207, an oral calcitonin gene related peptide receptor antagonist. Li CC, Vermeersch S, Denney WS, Kennedy WP, Palcza J, Gipson A, Han TH, Blanchard R, De Lepeleire I, Depré M, Murphy MG, Van Dyck K, de Hoon JN.Br J Clin Pharmacol. 2015 May;79(5):831-7. doi: 10.1111/bcp.12547. PMID: 25377933 Free PMC Article
2:Randomized controlled trial of the CGRP receptor antagonist MK-3207 in the acute treatment of migraine. Hewitt DJ, Aurora SK, Dodick DW, Goadsby PJ, Ge YJ, Bachman R, Taraborelli D, Fan X, Assaid C, Lines C, Ho TW.Cephalalgia. 2011 Apr;31(6):712-22. doi: 10.1177/0333102411398399. Epub 2011 Mar 7. PMID: 21383045
3:Discovery of MK-3207: A Highly Potent, Orally Bioavailable CGRP Receptor Antagonist. Bell IM, Gallicchio SN, Wood MR, Quigley AG, Stump CA, Zartman CB, Fay JF, Li CC, Lynch JJ, Moore EL, Mosser SD, Prueksaritanont T, Regan CP, Roller S, Salvatore CA, Kane SA, Vacca JP, Selnick HG.ACS Med Chem Lett. 2010 Jan 12;1(1):24-9. doi: 10.1021/ml900016y. eCollection 2010 Apr 8. PMID: 24900170 Free PMC Article
4:Pharmacological properties of MK-3207, a potent and orally active calcitonin gene-related peptide receptor antagonist. Salvatore CA, Moore EL, Calamari A, Cook JJ, Michener MS, O/’Malley S, Miller PJ, Sur C, Williams DL Jr, Zeng Z, Danziger A, Lynch JJ, Regan CP, Fay JF, Tang YS, Li CC, Pudvah NT, White RB, Bell IM, Gallicchio SN, Graham SL, Selnick HG, Vacca JP, Kane SA.J Pharmacol Exp Ther. 2010 Apr;333(1):152-60. doi: 10.1124/jpet.109.163816. Epub 2010 Jan 11. PMID: 20065019 Free Article