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AR-M 1896
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。
AR-M 1896图片
CAS NO:367518-31-8
包装:1mg
市场价:3959元

产品介绍
Selective GAL2 agonist
Cas No.367518-31-8
Canonical SMILESCC(C[C@@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/C/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](N)([H])CC1=CNC2=CC=CC=C12)([H])[C@@](O)([H])C)([H])CC(C)C)([H])CC(O)=N)([H])CO)([H])C)([H])CC3=CC=C(O)C=C3)([H])CC(C)C)([H])C(O)=N)C
分子式C54H81N13O14
分子量1136.31
溶解度Soluble to 1 mg/ml in 20% formic acid
储存条件Desiccate 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

Binding IC50: 1.76 nM for rGalR2; 879 nM for hGalR1

Galanin is a 29-aa neuropeptide with a complex role in pain processing. Galanin receptor subtypes are present in dorsal root ganglia and spinal cord with a differential distribution. Three galanin receptors, GalR1, GalR2 and GalR3, have been identified and cloned. AR-M1896 is a specific galanin R2 (GalR2) agonist.

In vitro: Additional removal of the glycine residue in position 1 resulted in AR-M1896 with almost unchanged GalR2 affinity and functional activity, and 500-fold selectivity for GalR2-Rs over GalR1-Rs. This compound represents a truly GalR2-selective galanin analog and, thus, could be used as a pharmacological tool to differentiate between these two receptors [1].

In vivo: In normal rats mechanical and cold allodynia of the hindpaw are induced by intrathecal infusion of low-dose galanin. The same effect is seen with equimolar doses of AR-M1896 or AR-M961 (an agonist both at GalR1 and GalR2 receptors). In allodynic Bennett model rats, the mechanical threshold dose-dependently increased after intrathecal injection of a high AR-M961dose, whereas no effect was observed in the control or AR-M1896 group. No effect of either compounds was observed in nonallodynic Bennett model rats [1].

Clinical trial: Up to now, AR-M1896 is still in the preclinical development stage.

Reference:
[1] Liu HX, Brumovsky P, Schmidt R, Brown W, Payza K, Hodzic L, Pou C, Godbout C, Hokfelt T. 
Receptor subtype-specific pronociceptive and analgesic actions of galanin in the spinal cord: selective actions via GalR1 and GalR2 receptors.  Proc Natl Acad Sci U S A. 2001 Aug 14;98(17):9960-4.