EPPTB|cas 1110781-88-8|DC Chemicals

Cas No.:	1110781-88-8
Chemical Name:	Ro 5212773
Synonyms:	EPPTB;N-(3-Ethoxy-phenyl)-4-pyrrolidin-1-yl-3-trifluoromethyl-benzamide;RO5212773;Ro 5212773;N-(3-Ethoxyphenyl)-4-pyrrolidin-1-yl-3-trifluoromethyl-benzamide;N-(3-ethoxyphenyl)-4-(pyrrolidin-1-yl)-3-(trifluoromethyl)benzamide;GTPL5457;EPPTB, >=95% (HPLC);BDBM50336205;n-(3-ethoxy-phenyl)-4-pyrrolidin-1-yl-3-trifluoro-methyl-benzamide;(N-(3-Ethoxy-phenyl)-4-pyrrolidin-1-yl-3-trifluoromethyl-benzamide;N-(3-Ethoxyphenyl)-4-(1-pyrrolidinyl)-3-(tr
SMILES:	FC(C1C=C(C(NC2C=CC=C(C=2)OCC)=O)C=CC=1N1CCCC1)(F)F
Formula:	C₂₀H₂₁F₃N₂O₂
M.Wt:	378.400
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	Ro 5212773 (EPPTB) is a potent and selective trace amine-associated receptor 1 (TAAR1) antagonist (Ki=0.9 nM for mouse TAAR1), with no significant effects on other TAARs. TAAR1 is a G protein-coupled receptor (GPCR) that is nonselectively activated by endogenous metabolites of amino acids[1][2].
In Vitro:	Ro 5212773 (EPPTB) suppresses the excitability of hippocampal pyramidal neurons. EPPTB also reduceds seizure-like events (SLEs) and seizure activity[1]. Ro 5212773 blocks the TAAR1-mediated activation of an inwardly rectifying K+ current[2]. Ro 5212773 potently antagonizes cAMP production induced by activating mouse TAAR1 with 1.5 μM β-phenylethylamine (IC50=27.5 nM). cAMP levels are dose-dependently reduced by Ro 5212773 in HEK293 cells in the absence of TAAR1 agonist (IC50= 19 nM). EPPTB is significantly more potent in antagonizing cAMP production by mouse, as compared to rat (IC50= 4539 nM) and human (IC50= 7487 nM) TAAR1[2].
References:	[1]. Bradaia A, et al. The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system. Proc Natl Acad Sci U S A. 2009;106(47):20081-20086.

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Ro 5212773