VU0361737 是一种高效选择性的，中枢神经系统渗透性的代谢型谷氨酸受体 4 (mGluR4)正变构调节剂，对人类和大鼠 mGluR4作用的EC50值分别为 240 和 110 nM。它具有神经保护作用，有用于帕金森氏病的研究潜力。

VU 0361737 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.

VU0361737 is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors and displays weak activity at mGlu5 and mGlu8 receptors. [1]

VU0361737 shows high in vivo CL in rat, a short half-life (T1/2 20 min), and demonstrates significant brain exposure (brain-to-plasma ratio of 4.1). [1]

Enzyme Assays: The enzymatic activities of NAMPT and NMNAT are measured using in vitro kits and using the Two-Step Method per manufacturer's instructions. Compounds, NAMPT and/or NMNAT enzymes, and their substrates are mixed and incubated at 30°C for 1 hour. Reagents for the indicator reaction (Wst-1) are then added, and absorbance is read at 450 nm every 5 min at 30°C on a Tecan In?nite M100 multimode plate reader.

1161205-04-4

C13H11ClN2O2

262.69

ML-128;VU 0361737

DMSO:26.3 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years