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首页-小分子抑制剂&激动剂-GPCR-Trace Amine-associated Receptor (TAAR)-EPPTB
EPPTB

Chemical Structure : EPPTB

CAS No.: 1110781-88-8

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EPPTB (Ro 5212773, RO5212773)

货号: PC-61073Not For Human Use, Lab Use Only.

EPPTB (Ro 5212773) is a potent, selective mouse TAAR1 antagonist that potently antagonizes cAMP production induced by 1.5 uM β-phenylethylamine with IC50 of 27.5 nM, Ki of 1 nM.

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

生物&药学活性

EPPTB (Ro 5212773) is a potent, selective mouse TAAR1 antagonist that potently antagonizes cAMP production induced by 1.5 uM β-phenylethylamine with IC50 of 27.5 nM, Ki of 1 nM.
EPPTB (Ro 5212773) displays >1,000-fold selectivity over dopamine, serotonin and adrenergic receptors.
EPPTB (Ro 5212773) dose-dependently reduces cAMP levels in HEK293 cells in the absence of TAAR1 agonist with IC50 of 19±12 nM, significantly more potent in antagonizing cAMP production by mouse, as compared to rat and human.
EPPTB (Ro 5212773)blocks the TAAR1-mediated activation of an inwardly rectifying K(+) current at dopamine (DA) neurons of the ventral tegmental area.

物理化学性质&存储条件

分子量 378.395
分子式 C20H21F3N2O2
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

N-(3-Ethoxy-phenyl)-4-pyrrolidin-1-yl-3-trifluoromethyl-benzamide

参考文献

1. Bradaia A, et al. Proc Natl Acad Sci U S A. 2009 Nov 24;106(47):20081-6.

2. Stalder H, et al. Bioorg Med Chem Lett. 2011 Feb 15;21(4):1227-31.

3. Leo D, et al. Neuropharmacology. 2014 Jun;81:283-91.

4. Liu X, et al. J Pharmacol Exp Ther. 2014 Jul;350(1):124-9.

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