Rac-VU 6008667 是毒蕈碱乙酰胆碱受体亚型 5 (M5 NAM) 的选择性负变构调节剂，对于人和大鼠的 IC50 值分别为 1.2 μM 和 1.6 μM。Rac-VU 6008667 具有高 CNS 渗透性。
| Cas No. | 2092917-63-8 |
| Canonical SMILES | O=C1N2C(N(C(C3=CC=C(F)C(F)=C3)=O)CC2)(C4=CC=C(Cl)C(C)=C4)C5=C1C=CC=C5 |
| 分子式 | C24H17ClF2N2O2 |
| 分子量 | 438.85 |
| 溶解度 | DMSO: 125 mg/mL (284.84 mM); Water:< 0.1 mg/mL (insoluble) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Rac-VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) with IC50s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. Rac-VU 6008667 has high CNS penetration[1]. M5 NAM: muscarinic acetylcholine receptor subtype 5. [1]. McGowan KM et al, Continued optimization of the M5 NAM ML375: Discovery of VU6008667, an M5 NAM with high CNS penetration and a desired short half-life in rat for addiction studies. Bioorg Med Chem Lett. 2017 Mar 15;27(6):1356-1359. |
