| Description | VU0361737 (ML-128) is a specific positive allosteric modulator (PAM) of mGlu4 receptor.The EC50 of VU 0361737 is 240 nM for the human receptors. The EC50 of VU 0361737 is110 nM for rat receptors.It exhibits weak activity at mGlu5 and mGlu8 receptors, and is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors, can penetrate into CNS. |
| In vitro | VU0361737 在mGlu1、mGlu2、mGlu3、mGlu6及mGlu7受体上无活性，并在mGlu5及mGlu8受体上表现出弱活性。[1] |
| In vivo | VU0361737 在大鼠体内显示出高清除率(CL)，半衰期短（T1/2 20分钟），并且显著地透过血脑屏障（脑血浆比率为4.1）。[1] |
| Target activity | mGluR4 (human):240 nM(EC50), mGluR4 (rat):110 nM(EC50) |
| Synonyms | ML-128, VU 0361737 |
| molecular weight | 262.69 |
| Molecular formula | C13H11ClN2O2 |
| CAS | 1161205-04-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 45 mg/mL (171.3 mM) |
| References | 1. Engers DW, et al. J Med Chem, 2009, 52(14), 4115-4118. 2. Engers DW, et al. J Med Chem, 2011, 54(4), 1106-1110. |