Ro 5212773 (EPPTB) 是一种有效和选择性的 (TAAR1) 拮抗剂(对于小鼠 TAAR1 的 K_i 值为 0.9 nM)，对其他 TAARs 没有显著影响。TAAR1 是一种 G 蛋白偶联受体 (GPCR)，由内源性氨基酸代谢产物非选择性激活。

Ro 5212773 (EPPTB) is a potent and selective trace amine-associated receptor 1 (TAAR1) antagonist (K i =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.

Solid

Ro 5212773 (EPPTB) suppresses the excitability of hippocampal pyramidal neurons. EPPTB also reduceds seizure-like events (SLEs) and seizure activity.
Ro 5212773 blocks the TAAR1-mediated activation of an inwardly rectifying K current.
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. has not independently confirmed the accuracy of these methods. They are for reference only.

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Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 100 mg/mL (264.28 mM; Need ultrasonic)配制储备液