| Description | JNJ-46281222 is an metabotropic glutamate (mGlu) 2-selective, highly potent PAM (positive allosteric modulator). It has nanomolar affinity (Kd = 1.7 nM) and a high modulatory potency (pEC50 = 7.71). |
| In vitro | Compared with WT, JNJ‐4628122 binds to the selected mGlu2?receptor mutants is significantly decreased by approximately 10‐fold. Mutations F643A and N735D are selected, in transfected mGlu2?WT and mutant receptors in CHO‐K1 cells [1]. |
| Target activity | mGluR2:1.7 nM (kd) |
| molecular weight | 414.47 |
| Molecular formula | C23H25F3N4 |
| CAS | 1254980-38-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 62.5 mg/mL (150.79 mM), Sonication is recommended. |
| References | 1. Doornbos ML,et al. Molecular mechanism of positive allosteric modulation of the metabotropic glutamate receptor 2 by JNJ-46281222.Br J Pharmacol. 2016 Feb;173(3):588-600. |