| Description | VU6012962 is an orally bioavailable negative allosteric modulator of CNS-penetrant metabotropic glutamate receptor 7(mGlu7; IC50: 347 nM). |
| In vitro | 与其他七种mGlu受体亚型相比,VU6012962对mGlu7具有高度选择性。 |
| In vivo | 在小鼠的升高零迷宫(EZM)实验中,VU6012962(剂量1-10 mg/kg;腹腔注射;测试前60分钟)能够降低焦虑。 |
| Target activity | mGlu7:347 nM |
| molecular weight | 448.4 |
| Molecular formula | C21H19F3N4O4 |
| CAS | 2313526-86-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 125 mg/mL (278.77 mM), Sonication is recommended. H2O: < 0.1 mg/mL (insoluble) |
| References | 1. Reed CW, et al. Discovery of an orally bioavailable and Central Nervous System (CNS) penetrant mGlu7 NegativeAllosteric Modulator (NAM) in vivo tool compound: N-(2-(1H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)-4-(cyclopropylmethoxy)-3-methoxybenzamide (VU6012962). J Med Chem. 2019 Jan 4. |