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MK-0974

CAS No. 781649-09-0

MK-0974 ( Telcagepant )

Catalog No. M15947 CAS No. 781649-09-0

A potent, selective, orally bioavailable CGRP receptor antagonist with Ki of 0.77 nM.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    MK-0974
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, selective, orally bioavailable CGRP receptor antagonist with Ki of 0.77 nM.
  • Description
    A potent, selective, orally bioavailable CGRP receptor antagonist with Ki of 0.77 nM; shows >10,000-fold selectivity in a panel of assays representing over 160 receptors, transporters, and enzymes; inhibits CGRP-stimulated cAMP production in E10 cells with IC50 of 2.2 nM; inhibits the capsaicin-induced increase in dermal blood flow in monkey models.Migraine Phase 3 Discontinued
  • Synonyms
    Telcagepant
  • Pathway
    GPCR/G Protein
  • Target
    CGRP Receptor
  • Recptor
    CGRP Receptor
  • Research Area
    Neurological Disease
  • Indication
    Migraine

Chemical Information

  • CAS Number
    781649-09-0
  • Formula Weight
    566.52
  • Molecular Formula
    C26H27F5N6O3
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    O=C(N1CCC(N(C2=CC=CN=C2N3)C3=O)CC1)N[C@H]4C(N(CC(F)(F)F)C[C@H](C5=CC=CC(F)=C5F)CC4)=O
  • Chemical Name
    1-Piperidinecarboxamide, 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)-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Paone DV, et al. J Med Chem. 2007 Nov 15;50(23):5564-7.
2. Salvatore CA, et al. J Pharmacol Exp Ther. 2008 Feb;324(2):416-21.
3. Sinclair SR, et al. Br J Clin Pharmacol. 2010 Jan;69(1):15-22.
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