| Description | VU 0469650 is a potent and selective negative allosteric modulator of mGluR1 (IC50 = 99 nM). |
| In vivo | VU 0469650(10 mg/kg;I.P.;一次性;雄性Sprague-Dawley大鼠)展现出极佳的选择性档案以及在血浆和大脑样本中良好的暴露度。VU 0469650(0.2 mg/kg;I.V.;一次性;雄性Sprague-Dawley大鼠)显示出中等至高的清除率,中等的分布体积,以及约1小时的半衰期。 |
| Target activity | mGlu1:99 nM |
| Synonyms | VU0469650, VU 0469650, VU-0469650, VU 0469650 HCl |
| molecular weight | 364.48 |
| Molecular formula | C22H28N4O |
| CAS | 1443748-47-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Ethanol: 45.0 mg/mL (112.2 mM) DMSO: 90.0 mg/mL (224.5 mM) |
| References | 1. Lovell KM, et al. N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats. Bioorg Med Chem Lett. 2013;23(13):3713-3718. |