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CAS No.: 957118-49-9

MK-3207 Catalog No. CSN13170

Synonyms: Mk-3207

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	数量

400-920-2911

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tech@csnpharm.cn

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

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^[3].
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.
临床研究
NCT号适应症或疾病临床期招募状态预计完成时间地点
NCT00712725 - - Completed - -
NCT00548353 Migraine Disorders Phase 1 Completed - -
NCT00712725 Migraine Phase 2 Completed - -
参考文献

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00712725	-	-	Completed	-	-
NCT00548353	Migraine Disorders	Phase 1	Completed	-	-
NCT00712725	Migraine	Phase 2	Completed	-	-

[1] Hewitt DJ, Aurora SK, et al. Randomized controlled trial of the CGRP receptor antagonist MK-3207 in the acute treatment of migraine. Cephalalgia. 2011 Apr;31(6):712-22.
[2] Salvatore CA, Moore EL, et al. 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.
[3] Salvatore CA, Moore EL, Calamari A, Cook JJ, Michener MS, O'Malley S, Miller PJ, Sur C, Williams DL Jr, Zeng Z, Danziger A, Lynch JJ, Regan CP, Fay JF, Tang YS, Li CC, Pudvah NT, White RB, Bell IM, Gallicchio SN, Graham SL, Selnick HG, Vacca JP, Kane SA. 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. doi: 10.1124/jpet.109.163816. Epub 2010 Jan 11. PMID: 20065019.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
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

技术信息

CAS号

957118-49-9

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C31H29F2N5O3

运输

蓝冰

分子量

557.59

别名

Mk-3207

溶解度

DMSO	100.0 mg/mL (179.3 mM)

动物实验配方

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