A CGRP receptor antagonist
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MK-3207

Item No. 42490

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
8R-(3,5-difluorophenyl)-10-oxo-N-[(2R)-1,1',2',3-tetrahydro-2'-oxospiro[2H-indene-2,3'-[3H]pyrrolo[2,3-b]pyridin]-5-yl]-6,9-diazaspiro[4.5]decane-9-acetamide
CAS Number
957118-49-9
Molecular Formula
C31H29F2N5O3
Formula Weight
557.6
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly Soluble: 0.1-1 mg/mlDMSO: Sparingly Soluble: 1-10 mg/ml
SMILES
O=C1[C@]2(CC3=CC(NC(CN4[C@H](C5=CC(F)=CC(F)=C5)CNC6(CCCC6)C4=O)=O)=CC=C3C2)C7=CC=CN=C7N1
InChi Code
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)/t25-,30+/m0/s1
InChi Key
AZAANWYREOQRFB-SETSBSEESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $47

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    5 mg

    $208

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    10 mg

    $347

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    Product Description

    MK-3207 is an antagonist of the calcitonin gene-related peptide (CGRP) receptor (Ki = 22 pM for the recombinant human receptor).1 It is selective for the CGRP receptor over adrenomedullin receptor 1 (AM1) and AM2, calcitonin (CT) receptor, and amylin 3 receptor (AMY3; Kis = 16.5, 0.156, 1.9, and 0.128 µM, respectively) but does inhibit AMY1 to a lesser extent (Ki = 750 pM). MK-3207 inhibits CGRP-induced cAMP production in HEK293 cells expressing the human CGRP receptor (IC50 = 120 pM). It decreases capsaicin-induced forearm dermal vasodilation in rhesus monkeys in a dose-dependent manner.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Salvatore, C.A., Moore, E.L., Calamari, A., et al. Pharmacological properties of MK-3207, a potent and orally active calcitonin gene-related peptide receptor antagonist. J. Pharmacol. Exp. Ther. 333(1), 152-160 (2010).