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TDZD-8  ≥98% (HPLC)

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包装规格：5mg 25mg 100mg in glass bottle
溶解性：溶于DMSO( >10 mg/mL )
产品描述：基本信息 产品编号： T80005 产品名称： TDZD-8  CAS: 327036-89-5   储存条件 粉末 2-8℃ 四年     分子式： C10H10N2O2S 溶于液体 -80℃ 6个月 分子量： 222.26 -20℃ 1个月 化学名：  4-Benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione Solubility (25°C)：   体外:   DMSO 44.5mg/mL (200.21mM) Ethanol 44.5mg/mL (200.21mM) Water Insoluble 体内(现配现用): 1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility:≥2.5mg/mL(11.25mM);Clear solution 此方案可获得 ≥ 2.5 mg/mL (11.25 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2.请依序添加每种溶剂：10% DMSO→90%(20% SBE-β-CD in saline) Solubility:≥2.5mg/mL(11.25mM);Clear solution 此方案可获得 ≥ 2.5 mg/mL (11.25 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3.请依序添加每种溶剂：10% DMSO→90% corn oil Solubility:≥2.5mg/mL(11.25mM);Clear solution 此方案可获得 ≥ 2.5 mg/mL (11.25 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀 ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 4.4992mL 22.4962mL 44.9924mL 5mM 0.8998mL 4.4992mL 8.9985mL 10mM 0.4499mL 2.2496mL 4.4992mL   生物活性 产品描述 一种选择性的GSK-3抑制剂。 靶点 GSK-3β 2μM (IC50)   体外研究 TDZD8 results in a significant decline of cellular ATP levels in PC-3 cells.TDZD8 (10μM) treatment also triggers a drastic autophagy response and AMPK activation in PC-3 cells.Furthermore,TDZD8 (10μM) reduces mTOR phosphorylation levels at the S2448 site.In addition,TDZD8 (10μM) induces LKB1 nuclear-cytoplasm translocation. 体内研究 TDZD-8 (TDZD8,1 or 2mg/kg,i.p.) both reduces the induction of p-DARPP32 following chronic L-dopa treatment in parkinsonian animals.TDZD8 treatment of 21 days induces a significant reduction in PKA expression in rats with established dyskinesia.Moreover,TDZD8 reduces FosB mRNA level in the striatum and lowers the expression of PPEB mRNA to similar levels as in 6-OHDA-lesioned rats without treated with L-dopa.The decrease in dyskinesia induced by TDZD8 is overcome by dopamine rceptor-1 agonist.   推荐实验方法(仅供参考) 激酶实验： GSK-3 activity is assayed in 50 mM Tris-HCl, pH 7.5,10mM MgCl2,1mM EGTA,and 1mM EDTA buffer,at 37℃,in the presence of 15μM GS-1 (substrate),15μM [γ-32P]ATP in a final volume of 12μL.After 20 min incubation at 37℃,4μL aliquots of the supernatant are spotted onto 2×2 cm pieces of Whatman P81 phosphocellulose paper, and 20s later,the filters are washed four times (for at least 10 min each time) in 1% phosphoric acid.The dried filters are transferred into scintillation vials,and the radioactivity is measured in a liquid scintillation counter.Blank values are subtracted,and the GSK-3β activity is expressed in picomoles of phosphate incorporated in GS-1 per 20 min or in percentage of maximal activity.   动物实验:   Apomorphine hydrochloride is administered (0.5mg/kg).L-dopa (25mg/kg) plus benserazide-HCl (6.25mg/kg) are given once-daily.TDZD8,a non-ATP competitive inhibitor of GSK-3β,is dissolved in 10% DMSO and is administered i.p.(TDZD8-L group,1mg/kg;TDZD8-H group,2mg/kg,respectively) 30 min prior to L-dopa intake for 3 weeks.(±)-1-Phenyl-2,3,4,5-tetrahydro-(1H)-3-benzazepine-7,8-diol hydrochloride (SKF38393),a D1 Dopamine receptor agonist,is dissolved in saline and is administered i.p.(SKF38393-L group,5mg/kg;SKF38393-H group,10mg/kg,respectively) 30 min prior to L-dopa intake for 3 weeks.
保存条件：2-8℃

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