Talampanel-GYKI-53773-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETalampanelCat. No.: HY-15079CAS No.: 161832-65-1Synonyms: GYKI-53773; LY-300164分式: CHNO分量: 337.37作靶点: iGluR; Apoptosis作通路: Membrane Transporter/Ion Channel; Neuronal Signaling;Apoptosis储存式: Powder -20C 3 years4C 2 yearsIn solven

2、t -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (296.41 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.9641 mL 14.8205 mL 29.6410 mL5 mM 0.5928 mL 2.9641 mL 5.9282 mL10 mM 0.2964 mL 1.4821 mL 2.9641 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。

3、体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.41 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)1/2 Master of Small M

4、olecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (7.41 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Talampanel (LY300164)种服和选择型 AMPA 受体拮抗剂，具有抗癫痫活性。Talampanel (IVAX) 具有神经保护作 (啮齿动物的中风模型中)。Talampanel 减弱 caspase-3 依赖性细胞凋亡 (apoptosis)。体内研究 Talampanel (orally administration; 5 mg/kg; once a day; 2 weeks) re

5、duces motoneuronal calcium in a mousemodel of ALS, but its efficacy declines as the disease progresses 1.Animal Model: Female mutant SOD1 Tg mice 1Dosage: 5 mg/kgAdministration: Orally administration; 5 mg/kg; once a day; 2 weeksResult: Had a significant effect in reducing the calcium level only at

6、the age of 12 weeks.REFERENCES1. Paizs M, et al. Talampanel reduces the level of motoneuronal calcium in transgenic mutant SOD1 mice only if appliedpresymptomatically. Amyotroph Lateral Scler. 2011 Sep;12(5):340-4.2. Denes L, et al. Talampanel a non-competitive AMPA-antagonist attenuates caspase-3 dependent apoptosis in mouse brain aftertransient focal cerebral ischemia. Brain Res Bull. 2006 Jul 31;70(3):260-2. Epub 2006 Mar 31.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.