A CGRP receptor antagonist
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MK-0974

Item No. 23960

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(3R,6S)-6-(2,3-difluorophenyl)hexahydro-2-oxo-1-(2,2,2-trifluoroethyl)-1H-azepin-3-yl]-4-(2,3-dihydro-2-oxo-1H-imidazo[4,5-b]pyridin-1-yl)-1-piperidinecarboxamide
CAS Number
781649-09-0
Molecular Formula
C26H27F5N6O3
Formula Weight
566.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 10 mMEthanol: 1 mg/ml
λmax
293 nm
SMILES
O=C(N[C@@H]1CC[C@@H](C2=CC=CC(F)=C2F)CN(CC(F)(F)F)C1=O)N3CCC(N4C(NC5=C4C=CC=N5)=O)CC3
InChi Code
InChI=1S/C26H27F5N6O3/c27-18-4-1-3-17(21(18)28)15-6-7-19(23(38)36(13-15)14-26(29,30)31)33-24(39)35-11-8-16(9-12-35)37-20-5-2-10-32-22(20)34-25(37)40/h1-5,10,15-16,19H,6-9,11-14H2,(H,33,39)(H,32,34,40)/t15-,19-/m1/s1
InChi Key
CGDZXLJGHVKVIE-DNVCBOLYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $75

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    5 mg

    $333

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    10 mg

    $589

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    Product Description

    MK-0974 is an orally bioavailable antagonist of the calcitonin gene-related peptide (CGRP) receptor complex (Ki = 0.77 μM), which is composed of the calcitonin receptor-like receptor (CRLR) and receptor activity modifying protein 1 (RAMP1).1 MK-0974 binds selectively to the human CGRP receptor complex, over the adrenomedullin receptor complexes, which are composed of CRLR and RAMP2 or RAMP3 (Kis = >100 and 29 μM, respectively, in HEK293 cells). MK-0974 also binds to rhesus, canine, and rat CGRP receptor complexes (Kis = 1.2, 1,204, and 1,192 nM, respectively). MK-0974 inhibits cAMP accumulation stimulated by CGRP (Item No. 24405) with an IC50 value of 2.2 nM in HEK293 cells expressing the CGRP receptor complex. Ex vivo, MK-0974 (5 μM) reduces CGRP-induced vasodilation in isolated human meningeal arteries.2 MK-0974 also inhibits vasodilation induced by topical application of capsaicin (Item No. 92350) in rhesus monkeys (EC50 = 127 nM).1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Salvatore, C.A., Hershey, J.C., Corcoran, H.A., et al. Pharmacological characterization of MK-0974 [N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide], a potent and orally active calcitonin gene-related peptide receptor antagonist for the treatment of migraine. J. Pharmacol. Exp. Ther. 324(2), 416-421 (2008).

    2. Grände, G., Labruijere, S., Haanes, K.A., et al. Comparison of the vasodilator responses of isolated human and rat middle meningeal arteries to migraine related compounds. J. Headache Pain 15, 22 (2014).