Talampanel-GYKI-53773-DataSheet-生命科學試劑-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作靶點: iGluR; Apoptosis作通路: Membrane Transporter/Ion Channel; Neuronal Signaling;Apoptosis儲存式: Powder -20C 3 years4C 2 yearsIn solven

2、t -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 100 mg/mL (296.41 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。

3、體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.41 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)1/2 Master of Small M

4、olecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (7.41 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Talampanel (LY300164)種服和選擇型 AMPA 受體拮抗劑，具有抗癲癇活性。Talampanel (IVAX) 具有神經(jīng)保護作 (嚙齒動物的中風模型中)。Talampanel 減弱 caspase-3 依賴性細胞凋亡 (apoptosis)。體內(nèi)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.