CAS:957118-49-9MK-3207

您的位置 : 首页 / Neuronal Signaling / CGRP Receptor / MK-3207

MK-3207 Cat No. FB03064Cas No. 957118-49-9

MK-3207 is a potent and orally bioavailable CGRP receptor antagonist (IC50= 0.12 nM; Ki value= 0.024 nM), showing highly selective versus human AM1, AM2, CTR, and AMY3.

规格	价格	促销价格	库存

18817579266

立即询价

咨询

18817579266

立即询价

实验数据

储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7934 mL
- 8.9672 mL
- 17.9343 mL
- 5 mM
- 0.3587 mL
- 1.7934 mL
- 3.5869 mL
- 10 mM
- 0.1793 mL
- 0.8967 mL
- 1.7934 mL
计算器摩尔计算器总药量计算器工作液计算器

技术信息

CAS号

957118-49-9

储存条件

粉末: -20°C 3 年

液体: -80°C 12 月

分子式

C31H29F2N5O3

运输

蓝冰

分子量

557.59

别名

溶解度

DMSO	100.0 mg/mL (179.3 mM)

动物实验配方

靶点数据

生物活性

描述Calcitonin gene-related peptide (CGRP) is a 37-amino acid neuropeptide involved in the pathophysiology of migraine. MK-3207 is a potent, orally bioavailable CGRP receptor antagonist. It exhibited high affinity for recombinant human receptor and for native human CGRP receptor in SK-N-MC cells with K_i values of 0.022 and 0.024nM, respectively. MK-3207 also displayed a similar affinity for rhesus monkey receptor with a K_i value of 0.024nM. In HEK293 cells expressing human CGRP receptor, MK-3207 inhibited human α-CGRP-stimulated cAMP responses with an IC50 value of 0.12±0.02nM. MK-3207 dose-dependently inhibited capsaicin-induced dermal blood flow in the rhesus monkey forearm with EC₅₀ and EC₉₀ values of 0.8 and 7nM, respectively. The IC50 value of MK-3207 in the human serum-shifted in vitro functional assay was 17nM.
作用机制MK-3207 is a potent, highly selective, and orally bioavailable antagonist of human and rhesus monkey CGRP receptors. The receptor activity-modifying protein 1 (RAMP1) is a transmembrane-spanning protein responsible for the regulation of CGRP activity. The residue 74 on RAMP1 plays a key role in MK-3207 binding to CGRP receptor.