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MK-3207 (Hydrochloride)

CAS No. 957116-20-0

MK-3207 (Hydrochloride) ( MK3207 Hydrochloride | MK 3207 Hydrochloride | MK-3207 )

产品货号. M16836 CAS No. 957116-20-0

一种高效、选择性 CGRP 受体拮抗剂,体外结合测定中的 Ki 为 21 pM,基于细胞的功能测定中的 IC50 为 0.12 nM。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
5MG ¥1134 有现货
10MG ¥2074 有现货
25MG ¥3507 有现货
50MG ¥5646 有现货
100MG ¥8068 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-3207 (Hydrochloride)
  • 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
    一种高效、选择性 CGRP 受体拮抗剂,体外结合测定中的 Ki 为 21 pM,基于细胞的功能测定中的 IC50 为 0.12 nM。
  • 产品描述
    A highly potent, selective CGRP receptor antagonist with Ki of 21 pM in in vitro binding assay and IC50 of 0.12 nM in cell-based functional assay; displays >50000-fold selectivity in a panel of 160 enzymes, receptors, channels, and 65-fold more potent than telcagepant; orally bioavailable.
  • 体外实验
    MK-3207 displays a similar affinity (Ki) for the rhesus monkey receptor (0.024±0.001 nM; n=14) as for human, but it displays >400-fold lower affinity for the canine and rat receptors, with values of 10 nM and 10±1.2 nM, respectively. MK-3207 is highly selective versus the human AM1 (CLR/RAMP2) and AM2 (CLR/RAMP3) receptors, with Ki values of 16,500 nM and 156±17 nM, respectively. MK-3207 maintains a high degree of selectivity versus human CTR, with a Ki value of 1.9±0.58 μM. MK-3207 also displays good selectivity versus the AMY3 (CTR/RAMP3) receptor, with a Ki value of 128±25 nM, but it is less selective versus the AMY1 (CTR/RAMP1) receptor, with a Ki value of 0.75±0.13 nM. MK-3207 potently blocks human α-CGRP-stimulated cAMP responses in human CGRP receptor-expressing HEK293 cells, with an IC50 value of 0.12±0.02 nM. MK-3207 displays significantly lower potency for the rat CGRP receptor, with a pIC50=7.31±0.09.
  • 体内实验
    MK-3207 is CNS-penetrant and therefore significantly engaging central receptors. After an oral dose of 10 mg/kg MK-3207, the CSF/plasma ratio is 2 to 3%.
  • 同义词
    MK3207 Hydrochloride | MK 3207 Hydrochloride | MK-3207
  • 通路
    GPCR/G Protein
  • 靶点
    CGRP Receptor
  • 受体
    CGRP
  • 研究领域
    Neurological Disease
  • 适应症
    ——

化学信息

  • CAS Number
    957116-20-0
  • 分子量
    594.0514
  • 分子式
    C31H30ClF2N5O3
  • 纯度
    >98% (HPLC)
  • 溶解度
    10 mM in DMSO
  • SMILES
    C1CCC2(C1)C(=O)N(C(CN2)C3=CC(=CC(=C3)F)F)CC(=O)NC4=CC5=C(CC6(C5)C7=C(NC6=O)N=CC=C7)C=C4.Cl
  • 化学全称
    6,9-Diazaspiro[4.5]decane-9-acetamide, 8-(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]-, hydrochloride (1:1), (8R)-

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. Bell IM, et al. ACS Med Chem Lett. 2010 Jan 12;1(1):24-9. 2. Salvatore CA, et al. J Pharmacol Exp Ther. 2010 Apr;333(1):152-60. 3. Li CC, et al. Br J Clin Pharmacol. 2015 May;79(5):831-7.
产品手册
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  • MK-3207

    一种高效、选择性 CGRP 受体拮抗剂,体外结合测定中的 Ki 为 21 pM,基于细胞的功能测定中的 IC50 为 0.12 nM。