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AR-M 1896

Catalog No.
B5328
Selective GAL2 agonist
Grouped product items
SizePriceStock Qty
1mg
$415.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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, Hökfelt 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.

Chemical Properties

Physical AppearanceWhite lyophilised solid
StorageDesiccate at -20°C
M.Wt1136.31
Cas No.367518-31-8
FormulaC54H81N13O14
SolubilitySoluble to 1 mg/ml in 20% formic acid
SDFDownload SDF
Canonical SMILESCC(C[[email protected]@](/N=C(O)/[[email protected]](/N=C(O)/[[email protected]](/N=C(O)/C/N=C(O)/[[email protected]](/N=C(O)/[[email protected]](/N=C(O)/[[email protected]](/N=C(O)/[[email protected]](/N=C(O)/[[email protected]](/N=C(O)/[[email protected]](N)([H])CC1=CNC2=CC=CC=C12)([H])[[email protected]@](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
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

AR-M 1896