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首页-小分子抑制剂&激动剂-GPCR-CGRP Receptor-Atogepant
Atogepant

Chemical Structure : Atogepant

CAS No.: 1374248-81-3

Atogepant (MK-8031, AGN-241689)

货号: PC-60031Not For Human Use, Lab Use Only.

Atogepant (MK-8031) is a potent and selective calcitonin gene-related peptide (CGRP) receptor antagonist with Ki of 2 pM (hCGRP).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Atogepant (MK-8031) is a potent and selective calcitonin gene-related peptide (CGRP) receptor antagonist with Ki of 2 pM (hCGRP).
Atogepant shows similar affinity for rhesus CGRP receptors (Ki = 0.009 nM), but a weaker affinity for rat and dog CGRP receptors (Ki = 0.7 nM and Ki = 1.2 nM, respectively).
Atogepant inhibited [125I]-amylin binding on membranes from cells expressing human recombinant AMY1 (Ki=1.8 nM).
Atogepant inhibited AMY-induced cAMP accumulation with an IC50 of 2.4 nM on the AMY1 receptor, and an IC50 of 1418 nM on the AMY3 receptor.
Atogepant exhibited significant affinity for the amylin1 receptor but lacked appreciable affinities for adrenomedullin, calcitonin and other known neurotransmitter receptor targets.
Atogepant dose-dependently inhibited facial allodynia in the rat nitroglycerine model and produced significant CIDV inhibition in primates.

物理化学性质&存储条件

分子量 603.525
分子式 C29H23F6N5O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(3'S)-N-[(3S,5S,6R)-6-methyl-2-oxo-1-(2,2,2-trifluoroethyl)-5-(2,3,6-trifluorophenyl)piperidin-3-yl]-2'-oxo-1',2',5,7-tetrahydrospiro[cyclopenta[b]pyridine-6,3'-pyrrolo[2,3-b]pyridine]-3-carboxamide

参考文献

1. Rubio-Beltran E, et al. Cephalalgia. 2020 Apr;40(4):357-366.

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