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VU 0361737
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
VU 0361737图片
CAS NO:1161205-04-4
包装与价格：
包装价格(元)
10mg电议
50mg电议

产品介绍
VU 0361737 (ML-128) 是一种强效、选择性和 CNS 渗透性正向变构调节剂，作用于代谢型谷氨酸受体 4 (mGluR4 PAM)，对人和大鼠 mGluR4 受体的 EC50 分别为 240 nM 和 110 nM。
Cas No.1161205-04-4
别名ML-128
化学名N-(4-chloro-3-methoxyphenyl)pyridine-2-carboxamide
Canonical SMILESCOC1=C(C=CC(=C1)NC(=O)C2=CC=CC=N2)Cl
分子式C13H11ClN2O2
分子量262.69
溶解度DMF: 50 mg/ml,DMSO: 50 mg/ml,DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml,Ethanol: 10 mg/ml
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

VU0361737 is a selective, positive allosteric modulator and brain-permeable for mGLuR4 (mGlu4 receptor), (EC50 = 240 and 110 nM for human and rat receptors respectively), >50 fold selectivity over other mGluR subtypes. Inactive at mGluR-1, mGluR-2, mGluR-3, mGluR-6 and mGluR-7 receptors and showed weak activity at mGluR-5 and mGluR-8 receptors. [1]

The mGluR (metabotropic glutamate receptor) is a group of G-protein coupled receptors and is active through an indirect metabotropic process. mGLuR4 are invoinved in Parkinson as it decrease GABAerigic transmission at inhibitory striato-pallidal synapse with the basal ganglia.[1][2]

Following the administration of VU0361737 into rat intraperitoneally (10mg/kg), the amount of compound present in brain and plasma was determined at 0.5, 1 and 8 hours. It showed a short half-life (T1/2 20 minutes) and a pronounced brain exposure (brain: plasma ratio = 4.1) [1]

References:
[1] Engers DW, Niswender CM, Weaver CD, Jadhav S, Menon UN, Zamorano R, Conn PJ, Lindsley CW, Hopkins CR.  Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs).  J Med Chem. 2009 Jul 23;52(14):4115-8. 
[2] Engers DW, Field JR, Le U, Zhou Y, Bolinger JD, Zamorano R, Blobaum AL, Jones CK, Jadhav S, Weaver CD, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR.  Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats.  J Med Chem.  2011 Feb 24;54(4):1106-10.