Ro 5212773 (EPPTB)是一种高效且选择性的痕胺相关受体 1 (TAAR1) 拮抗剂,对小鼠 TAAR1 的 Ki 值为 0.9 nM,且对其他 TAAR 受体无显著影响。
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描述 | Ro 5212773, also known as EPPTB, is a potent and selective TAAR1 antagonist (Ki=0.9 nM for mouse TAAR1) and has no significant effect on other TAARs[1][2].Ro 5212773 inhibits excitability of hippocampal pyramidal neurons and also reduces seizure-like events (SLE) and seizure activity[1].Ro 5212773 blocked TAAR1-mediated inwardly rectifying K+ current activation. Ro 5212773 effectively antagonised 1.5 μM β-phenylethylamine activation of cAMP production induced by TAAR1 in mice (IC50= 27.5 nM). The antagonistic effect of Ro 5212773 on cAMP production in mice was significantly stronger compared to TAAR1 in rat (IC50= 4539 nM) and human (IC50= 7487 nM)[2]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.64mL 0.53mL 0.26mL |
13.21mL 2.64mL 1.32mL |
26.43mL 5.29mL 2.64mL |
CAS号 | 1110781-88-8 |
分子式 | C20H21F3N2O2 |
分子量 | 378.39 |
SMILES Code | O=C(C1=CC=C(C(C(F)(F)F)=C1)N2CCCC2)NC3=CC=CC(OCC)=C3 |
MDL No. | MFCD21605509 |
别名 | EPPTB |
运输 | 蓝冰 |
InChI Key | KLFVWQCQUXXLOU-UHFFFAOYSA-N |
Pubchem ID | 25175634 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry, 2-8°C |
溶解方案 |
DMSO: 105 mg/mL(277.49 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的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
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