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MK-0974

CAS No. 781649-09-0

MK-0974 ( Telcagepant )

产品货号. M15947 CAS No. 781649-09-0

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

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
50MG ¥8068 有现货
100MG ¥12879 有现货
200MG 获取报价 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    MK-0974
  • 注意事项
    本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
  • 产品简述
    A potent, selective, orally bioavailable CGRP receptor antagonist with Ki of 0.77 nM.
  • 产品描述
    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
  • 同义词
    Telcagepant
  • 通路
    GPCR/G Protein
  • 靶点
    CGRP Receptor
  • 受体
    CGRP Receptor
  • 研究领域
    Neurological Disease
  • 适应症
    Migraine

化学信息

  • CAS Number
    781649-09-0
  • 分子量
    566.52
  • 分子式
    C26H27F5N6O3
  • 纯度
    >98% (HPLC)
  • 溶解度
    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
  • 化学全称
    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)-

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

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.
产品手册
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