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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-TRP Channel-AMG21629
AMG21629

Chemical Structure : AMG21629

CAS No.: 939040-79-6

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AMG21629 (AMG-21629)

货号: PC-49443Not For Human Use, Lab Use Only.

AMG21629 is a potent and selective TRPV1 antagonist, inhibits Ca2+ uptake by CHO cells expressing TRPV1 receptors with IC50 of 0.6 nM and 0.8 nM for capsaicin and acid-induced Ca2+ uptake, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

AMG21629 is a potent and selective TRPV1 antagonist, inhibits Ca2+ uptake by CHO cells expressing TRPV1 receptors with IC50 of 0.6 nM and 0.8 nM for capsaicin and acid-induced Ca2+ uptake, respectively.
AMG21629 displayss >4000-fold selectivity for TRPV1 over other TRP channels.
AMG21629 blocks capsaicin-induced flinch response and causes hyperthermia in rats.

物理化学性质&存储条件

分子量 472.428
分子式 C22H19F3N6O3
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-Amino-5-[[2-[(2-methoxyethyl)amino]-6-[4-(trifluoromethyl)phenyl]-4-pyrimidinyl]oxy]-2(1H)-quinoxalinone

参考文献

1. Nuria Tamayo, et al. J Med Chem. 2008 May 8;51(9):2744-57.

2. Matthew I Brier, et al. Sci Rep. 2020 Aug 4;10(1):13096.

3. Narender R Gavva, et al. J Neurosci. 2007 Mar 28;27(13):3366-74.

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