| Description | VU0357121, a positive allosteric modulator of mGlu5 (EC50: 33 nM), is inactive or very weakly antagonizing at other mGlu receptor subtypes. |
| In vitro | VU0357121不会与mGlu5的MPEP异构体结合位点结合，因此不具备mGlu5 NAM活性。A809V/rmGlu5突变抑制了VU0357121调节谷氨酸浓度-反应曲线的能力，而F585I/rmGlu5突变并未改变对VU0357121的反应。[1] 在表达量较低的HEK293A-mGlu5细胞系中，VU0357121在Ca2+动员实验中表现出较弱的协同性。[2] |
| Target activity | mGluR5:30 nM(EC50) |
| molecular weight | 305.32 |
| Molecular formula | C17H17F2NO2 |
| CAS | 433967-28-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Ethanol: 30.5 mg/mL (100 mM) DMSO: 30.5 mg/mL (100 mM) |
| References | 1. Hammond AS, et al. ACS Chem Neurosci, 2010, 1(10), 702-716. 2. Gregory KJ, et al. Mol Pharmacol, 2012 Aug 3. |