| CAS NO: | 1110781-88-8 |
EPPTB is a selective antagonist of the trace amine-associated receptor 1 (TAAR1), a G protein-coupled receptor (GPCR) activated by endogenous trace amines (tyramine, tryptamine, synephrine, octopamine, β)-phenylethylamine), which are chemically similar to monoaminergic neurotransmitters (epinephrine, norepinephrine, dopamine). TAAR1 is considered a promising target for the treatment of neuropsychiatric disorders, however study of TAAR1 has hampered by the fact that selective ligands have not been available. EPPTB is the first potent and selective TAAR1 antagonist with an IC50of 28 nM at mouse TAAR1. EPPTB is less selective for rat and human with IC50values of 4539 and 7487 nM, respectively.
| 分子量 | 378.39 |
| 分子式 | C20H21F3N2O2 |
| CAS号 | 1110781-88-8 |
| 纯度 | >98% |
| 溶解性（25°C） | DMSO: 20 mg/mL clear |
| 储存和运输条件 | 固体粉末： -20°C 冷藏长期储存 常温运输及临时存放 |
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.6428 mL | 13.2139 mL | 26.4278 mL |
| 5 mM | 0.5286 mL | 2.6428 mL | 5.2856 mL |
| 10 mM | 0.2643 mL | 1.3214 mL | 2.6428 mL |
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