MK-3207

• 常用名: MK-3207
• 英文名: MK-3207
• CAS号: 957118-49-9
• 分子量: 557.591
• 密度: 1.5±0.1 g/cm3
• 沸点: 812.1±65.0 °C at 760 mmHg
• 分子式: C₃₁H₂₉F₂N₅O₃
• 熔点: N/A
• 闪点: 444.9±34.3 °C

MK-3207用途

MK-3207是口服生物相容性的CGRP受体拮抗剂，IC50和Ki分别为0.12 nM和0.024 nM，对AM1，AM2，CTR和AMY3的抑制性较弱。

MK-3207名称

• 中文名: MK-3207
• 英文名: 2-[(8R)-8-(3,5-difluorophenyl)-10-oxo-6,9-diazaspiro[4.5]decan-9-yl]-N-[(2R)-2'-oxospiro[1,3-dihydroindene-2,3'-1H-pyrrolo[2,3-b]pyridine]-5-yl]acetamide

MK-3207生物活性

• 描述: MK-3207是口服生物相容性的CGRP受体拮抗剂,IC50和Ki分别为0.12 nM和0.024 nM,对AM1,AM2,CTR和AMY3的抑制性较弱。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> CGRP受体
  信号通路 >> 神经信号通路 >> CGRP受体
  研究领域 >> 神经疾病
• 参考文献:

  [1]. Salvatore CA, Moore EL, Calamari A, Pharmacological properties of MK-3207, a potent and orally active calcitonin gene-related peptide receptor antagonist. J Pharmacol Exp Ther. 2010 Apr;333(1):152-60.

  [2]. Hewitt DJ, Aurora SK, Dodick DW, Randomized controlled trial of the CGRP receptor antagonist MK-3207 in the acute treatment of migraine. Cephalalgia. 2011 Apr;31(6):712-22.

MK-3207物理化学性质

• 密度: 1.5±0.1 g/cm3
• 沸点: 812.1±65.0 °C at 760 mmHg
• 分子式: C₃₁H₂₉F₂N₅O₃
• 分子量: 557.591
• 闪点: 444.9±34.3 °C
• 精确质量: 557.223816
• PSA: 106.92000
• LogP: 4.87
• InChIKey: AZAANWYREOQRFB-BRUPJXTFSA-N
• SMILES: O=C(CN1C(=O)C2(CCCC2)NCC1c1cc(F)cc(F)c1)Nc1ccc2c(c1)CC1(C2)C(=O)Nc2ncccc21
• 蒸汽压: 0.0±2.9 mmHg at 25°C
• 折射率: 1.689
• 储存条件: 2-8℃

MK-3207靶点实验

查看更多实验

实验名称：Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident pro... 来源：NCGC 靶标：N/A External Id：SERCaMPGLuc-p1-antagonist

实验名称：Aqueous solubility of the compound in phosphate buffer at pH 7 来源：ChEMBL 靶标：N/A External Id：CHEMBL2040014

实验名称：Primary qHTS assay for inhibitors of alpha-synuclein gene (SNCA) expression 来源：NCGC External Id：SNCA-p-activity-luciferase

实验名称：Selectivity for human CGRP receptor over AMY1 receptor (unknown origin) 来源：ChEMBL 靶标：N/A External Id：CHEMBL3370776

实验名称：Primary qHTS for Identification of Small Molecule Activators of Huntingtin-Antisense ... 来源：NCGC External Id：huntington-HTTAS8-p1-FF-overN

实验名称：Selectivity for human CGRP receptor over AM3 receptor (unknown origin) 来源：ChEMBL 靶标：N/A External Id：CHEMBL3370775

实验名称：Antimigraine activity in iv dosed rat assessed as inhibition of capsaicin-induced der... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL2040009

实验名称：Displacement of [125I]CGRP from CGRP receptor in rat brain membrane after 3 hrs 来源：ChEMBL 靶标：Calcitonin gene-related peptide type 1 receptor External Id：CHEMBL2040006

实验名称：Fraction unbound in rat plasma 来源：ChEMBL 靶标：Plasma External Id：CHEMBL2040007

实验名称：Cytotoxicity counterscreen for inhibitors of SARS-CoV-2 cell entry 来源：NCGC 靶标：N/A External Id：TRND-SARS-CoV-2-cytotox-48hr

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MK-3207英文别名

• unii-5c44m1qycc
• mk-3207
• 2-[(8R)-8-(3,5-Difluorophenyl)-10-oxo-6,9-diazaspiro[4.5]dec-9-yl]-N-[(2R)-2'-oxo-1,1',2',3-tetrahydrospiro[indene-2,3'-pyrrolo[2,3-b]pyridin]-5-yl]acetamide