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ZJ 43
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。
ZJ 43图片
CAS NO:723331-20-2
包装:10mg
市场价:4337元

产品介绍
ZJ 43 是一种有效的 NAAG 肽酶抑制剂,IC50 为 2.4 nM,Ki 为 0.8 nM。
Cas No.723331-20-2
化学名(2S)-2-[[(1S)-1-carboxy-3-methylbutyl]carbamoylamino]pentanedioic acid
Canonical SMILESCC(C)CC(C(=O)O)NC(=O)NC(CCC(=O)O)C(=O)O
分子式C12H20N2O7
分子量304.3
溶解度<30.43mg/ml in Water;<30.43mg/ml in DMSO
储存条件Store at -20℃
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

IC50: 2.4 nM

ZJ-43 is a N-acetylaspartylglutamate (NAAG) peptidase inhibitor.

The peptide neurotransmitter N-acetylaspartylglutamate (NAAG) is reported to act as an agonist at group II metabotropic glutamate receptors. NAAG is inactivated by extracellular peptidase activity leading to yielding glutamate and N-acetylaspartate.

In vitro: As a potent inhibitor of glutamate carboxypeptidase II and III (GCP II and III) with Kivalues of 0.8 and 23 nM respectively, ZJ-43 inhibited the hydrolysis of NAAG via indirect interactions with NMDA or metabotropic glutamate receptors [1].

In vivo: Intravenous injection of ZJ-43 coiuld suppress both phases of the agitation behaviour induced by paw formalin injection in the rat neuropathic pain model. Moreover, intravenous administration of ZJ-43 attenuated the level of mechanical allodynia induced by the nerve ligation. These effects of ZJ-43 in both the formalin test and the partial sciatic nerve ligation model were completely antagonized by pretreatment with LY-341495, which was a highly selective group II mGluR antagonist [1].

Clinical trial: N/A

Reference:
[1] Yamamoto T1,Hirasawa S,Wroblewska B,Grajkowska E,Zhou J,Kozikowski A,Wroblewski J,Neale JH.  Antinociceptive effects of N-acetylaspartylglutamate (NAAG) peptidase inhibitors ZJ-11, ZJ-17 and ZJ-43 in the rat formalin test and in the rat neuropathic pain model. Eur J Neurosci.2004 Jul;20(2):483-94.