HT-2157-SNAP-37889-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEHT-2157Cat. No.: HY-100717CAS No.: 303149-14-6Synonyms: SNAP 37889分式: CHFNO分量: 366.34作靶点: Neuropeptide Y Receptor作通路: GPCR/G Protein; Neuronal Signaling储存式: 4C, stored under nitrogen* In solvent : -80C, 6 months; -20C, 1 month (

2、stored undernitrogen)溶解性数据体外实验 DMSO : 29 mg/mL (79.16 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.7297 mL 13.6485 mL 27.2970 mL5 mM 0.5459 mL 2.7297 mL 5.4594 mL10 mM 0.2730 mL 1.3649 mL 2.7297 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGIC

3、AL ACTIVITY物活性 HT-2157(SNAP 37889)种选择性的亲和丙肽-3 受体 (Gal3) 竞争性拮抗剂。IC50 & Target Galanin-3 receptor 1体外研究HT-2157 (SNAP 37889) binds with high affinity to membranes from transiently transfected LMTK- cellsexpressing the human Gal3 receptor (Ki=17.440.01 nM; n100) and is highly selective for Gal3 over the

4、1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEGal1 and Gal2 subtypes (Ki10,000 nM for each subtype; n=46 of each subtype). When tested for theantagonism of galanin-evoked inhibition of adenylyl cyclase, HT-2157 (0.1-10 M) produces concentration-dependent rightward shifts of the concentration-effe

5、ct curve to galanin 1.体内研究 The galanin-3 receptor antagonist, HT-2157 (SNAP 37889), reduces operant responding for ethanol inalcohol-preferring rats. The novel selective GALR3 antagonist, HT-2157, to reduce anxiety-like behaviourand voluntary ethanol consumption in the iP (alcohol-preferring) rat. M

6、ale iP rats treated with HT-2157 at adose of 30 mg/kg (i.p.) do not show altered locomotor activity or changes in anxiety-like behaviour in theelevated plus maze or light-dark paradigms. Treatment with HT-2157 (30 mg/kg, i.p.) reduces operantresponding for solutions containing ethanol, sucrose and s

7、accharin. Collectively, results from the currentstudy shows that HT-2157 (30 mg/kg, i.p.) is effective in reducing operant responding for ethanol,independent of a sedative effect 2.PROTOCOLKinase Assay 1 Binding affinities for HT-2157 (SNAP 37889) and SNAP 398299 at the human Gal1, Gal2, and Gal3rec

8、eptors are determined by using the 125I-galanin displacement assay. Additionally, is tested for binding ina broad cross-reactivity panel that included G-protein-coupled receptors, ion channels, enzymes, andtransporters. The ability of HT-2157 to antagonize functional responses to galanin is examined

9、 in modifiedHEK-293 cells (PEAKrapid cells) transiently cotransfected with the Gal3 receptor and Gz by measuring theinhibition of adenylyl cyclase activity 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats 2Administration 2 The effect of HT-

10、2157 on locomotor activity is examined using adult male iP rats (n=12; 418-467 g).Locomotor activity is tested to ensure that any potential change in anxiety or ethanol consumption insubsequent tests is not due to any sedative property of the drug. Rats are habituated to the locomotor cells(262640 c

11、m) for 60 minute sessions which are conducted daily for three consecutive days. To minimisethe effect of habituation during the treatment phase, rats are divided into two even groups which received asingle injection of either HT-2157 (30 mg/kg, i.p.) or vehicle (1 ml/kg i.p.) 30 min prior to being p

12、laced in thelocomotor cells for a 60 minute session. The following day the treatments are reversed so that all ratsreceived treatment with both the vehicle and SNAP 37889 compound. Movements in terms of number ofmoves, move time (s) and total distance travelled (cm), are recorded automatically using

13、 TruScan 2.0software.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Am J Pathol. 2019 Apr;189(4):886-899.See more customer validations on HYPERLINK / www.MedChemEREFERENCES2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE1. Swanson CJ, et a

14、l. Anxiolytic- and antidepressant-like profiles of the galanin-3 receptor (Gal3) antagonists SNAP 37889 and SNAP398299. Proc Natl Acad Sci U S A. 2005 Nov 29;102(48):17489-94.2. Ash BL, et al. The galanin-3 receptor antagonist, SNAP 37889, reduces operant responding for ethanol in alcohol-preferring rats. RegulPept. 2011 Jan 17;166(1