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抑制剂 > 神经科学 > VU 0364439
产品名称:
VU 0364439
型号:
CS-01Y77444
生产地址
进口、国产
产品价格
电议
产品简介
质量保证、价格优惠
产品详情

一、概述:

化学性质:                                                                                                             

规格

10mM (in 1mL DMSO) 5mg 25mg 100mg

CAS

1246086-78-1

别名

 

化学名

N-[3-chloro-4-[(2-chlorophenyl)sulfamoyl]phenyl]pyridine-2-carboxamide

分子式

C18H13Cl2N3O3S

分子量

422.29

溶解度

21.1mg/mL in DMSO

储存条件

Store at -20°C

General tips

For obtaining a higher solubility , please warm the tube at 37 and shake it in the ultrasonic bath for a while.

Shipping Condition

Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

 

产品描述:                                                                                                            

VU 0364439 is a positive allosteric modulator (PAM) of mGlu4 with an EC50 value of 19.8 nM [1] [2] [3].

MGlu4 belongs to metabotropic glutamate receptor (mGluR) group III which contains mGlu4, mGlu6, mGlu7 and mGlu8. MGluRs belong to Class C of G-protein-coupled receptor (GPCR) superfamily. GPCRs modulate postsynaptic effects or the release of glutamate [2].

VU 0364439 exhibited excellent in vitro maximal response and potency relative to another PAM, (−)-PHCCC (a partially selective mGlu4 potentiator, its chemical structure could be found in reference 4). Starting at 30µM, using a 1:3 serial dilutions, VU 0364439 was tested in triplicate. The entire test was performed on one day. Finally, the % (−)-PHCCC value of VU 0364439 was 102.3. The value of % (−)-PHCCC was computed through dividing the maximal response elicited by VU 0364439 by the response of the control PAM, (−)-PHCCC, on the same day. It was also found that the EC50 value of VU 0364439 was 19.8 nM at human mGlu4 [4].

VU 0364439 possessed less than ideal pharmacokinetic properties. The properties of VU 0364439 prevents VU 0364439 itself from being used as an in vivo tool, but VU 0364439 might inform the mGlu4 community with more in vitro tool compounds [4].

特别提醒:                                                                                                              

1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗,食品及化妆品等用途。请勿存放于普通住宅区。

2. 为了您的安全和健康,请穿好实验服并佩戴一次性手套和口罩操作。

标签:VU 0364439 

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