Ro 5212773 (EPPTB) is a potent and selectivetrace amine-associated receptor1(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 ofamino acids^[1][2].

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].

378.39

Solid

C₂₀H₂₁F₃N₂O₂

1110781-88-8

Room temperature in continental US; may vary elsewhere.

DMSO : 100 mg/mL(264.28 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.5 mg/mL (6.61 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (6.61 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。