Gabazine-SR95531-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGabazineCat. No.: HY-103533CAS No.: 104104-50-9Synonyms: SR95531分式: CHBrNO分量: 368.23作靶点: GABA Receptor作通路: Membrane Transporter/Ion Channel; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 mont

2、h溶解性数据体外实验 DMSO : 75 mg/mL (203.68 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.7157 mL 13.5785 mL 27.1569 mL5 mM 0.5431 mL 2.7157 mL 5.4314 mL10 mM 0.2716 mL 1.3578 mL 2.7157 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。BIOLOGICAL ACTIVITY物活性 Gaba

3、zine是GABAA 受体 的选择性竞争性拮抗剂，其对 GABA 受体的 IC50 值为 0.2 M。IC50 & Target 0.2 M (GABA receptor) 1.体外研究Both bicuculline and Gabazine (SR 95531) have been characterized as competitive inhibitors of GABA1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEbinding to the GABAA receptor. Gabazine is more potent than

4、bicuculline at blocking currents elicited byGABA, with an IC50 for currents elicited by 3 M GABA of 0.2 M and a Hill coefficient of 1.0. Gabazinereduces the currents elicited by 10 M alphaxalone by 30%, for responses of receptors containing wildtype2 subunits. The concentration of Gabazine requires

5、producing half the maximal block is 0.2 M. Gabazinealso could only produce a partial block of currents gated by 300 M pentobarbital. The maximal reduction,again, is 30%, and the concentration of Gabazine required to produce half the maximal block is 0.15 M1.REFERENCES1. Ueno S, et al. Bicuculline and gabazine are allosteric inhibitors of channel opening of the GABAA receptor. J Neurosci. 1997 Jan15;17(2):625-34.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-379