产品说明
生化/生理作用
RO5256390 is an orally available partial agonist that targets trace amine-associated receptor 1 (TAAR1) with high affinity (Ki in nM = 0.9/mouse, 4.1/human, 9.1/rat, 24/monkey TARR1), potency (EC50 in nM/relative efficacy with respect to β-phenylethylamine = 1.3/0.59/mouse, 17/0.81/human, 47/0.76/rat, 251/0.85/monkey TARR1-dependent cellular cAMP production), and selectivity (by a 112-receptor/channel/transporter and a 42-enzyme panel), without agonistic activity toward mouse TAAR4-expressing cells even at a high concentration of 30 μM. When applied via oral administration (0.003-1 mg/kg), RO5256390 exhibits similar in vivo efficacy as the full agonist RO5256390 in blocking psychostimulants-induced hyperlocomotion in mice.
基本信息
| 经验(实验)分子式 | C10H11FN2O |
| 分子量 | 194.21 |
| MDL编号 | MFCD28405323 |
| NACRES | NA.77 |
产品性质
| 测定 | ≥98% (HPLC) |
| 形式 | powder |
| 旋光性 | [α]/D +77 to +88°, c = 1.0 in methanol |
| 颜色 | white to beige |
| 溶解性 | DMSO: 2 mg/mL, clear |
| 储存温度 | 2-8℃ |
| SMILES string | NC1=N[C@@H](C2=CC=CC(F)=C2C)CO1 |
安全信息
| 储存分类代码 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
