M871

M871 (Galanin- (2-13) -Glu-His- (Pro) 3- (Ala-Leu) 2-Ala-amide) is an orally active and selective galanin receptor type 2 (GalR2) antagonist. M871 exhibits Ki values of 13.1 nM, 420 nM and >10 μM for GalR2, GalR1 and GalR3 respectively. M871 relieves the mice allergic rhinitis by reducing IgE production, as well as the number of B cells in tissues. M871 can inhibit the nerve invasion of salivary adenoid cystic carcinoma (SACC) and alleviate myocardial ischemia-reperfusion injury. M871 can be used for research on GalR2-related diseases (such as epilepsy, pain) [1][2][3][4][5][6][7].

Product Specifications

CAS Number

908844-75-7

Product Name Alternative

Galanin- (2-13) -Glu-His- (Pro) 3- (Ala-Leu) 2-Ala-amide

UNSPSC

12352209

Target

Neuropeptide Y Receptor

Type

Peptides

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Cancer; Endocrinology; Inflammation/Immunology; Neurological Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/m871.html

Purity

99.98

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C([C@H]1N(CCC1)C([C@@H](NC([C@H](CCC(O)=O)NC([C@H]2N(CCC2)C(CNC([C@H](CC(C)C)NC([C@H](CC(C)C)NC([C@@H](NC(CNC([C@H](C)NC([C@H](CO)NC([C@H](CC(N)=O)NC([C@H](CC(C)C)NC([C@H]([C@H](O)C)NC([C@@H](N)CC3=CNC4=CC=CC=C34)=O)=O)=O)=O)=O)=O)=O)CC5=CC=C(C=C5)O)=O)=O)=O)=O)=O)=O)CC6=CN=CN6)=O)N7[C@@H](CCC7)C(N8[C@@H](CCC8)C(N[C@@H](C)C(N[C@@H](CC(C)C)C(N[C@@H](C)C(N[C@@H](CC(C)C)C(N[C@@H](C)C(N)=O)=O)=O)=O)=O)=O)=O

Molecular Formula

C108H163N27O28

Molecular Weight

2287.61

References & Citations

[1]U. E. Sollenberg, et al. M871—A Novel Peptide Antagonist Selectively Recognizing the Galanin Receptor Type 2. Int J Pept Res Ther. 2006;12:2965-2982.|[2]Sollenberg, U.E., et al. Binding of Chimeric Peptides M617 and M871 to Galanin Receptor Type 3 Reveals Characteristics of Galanin Receptor–Ligand Interaction. Int J Pept Res Ther 16, 17–22 (2010) .|[3]Kawada M, Yokoi H, Kimura T, Matsumoto Y, Sakurai H, Matsumoto K, Fujiwara M, Saito K. Involvement of galanin and galanin receptor 2 in a mouse model of allergic rhinitis. Allergol Int. 2022 Jan;71 (1) :83-93.|[4]Serebryakova L, et al. Exogenous GalR2-specific peptide agonist as a tool for treating myocardial ischemia/reperfusion injury. Fundam Clin Pharmacol. 2023 Dec;37 (6) :1109-1118.|[5]Wang J, et al. The GAL/GALR2 axis promotes the perineural invasion of salivary adenoid cystic carcinoma via epithelial-to-mesenchymal transition. Cancer Med. 2023 Feb;12 (4) :4496-4509.|[6]Li M, et al. Galanin Receptor 2 Is Involved in Galanin-Induced Analgesic Effect by Activating PKC and CaMKII in the Nucleus Accumbens of Inflammatory Pain Rats. Front Neurosci. 2021 Jan 21;14:593331.|[7]Fang P, et al. Central galanin receptor 2 mediates galanin action to promote systemic glucose metabolism of type 2 diabetic rats. Biochem Pharmacol. 2018 Oct;156:241-247.