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H-89  ≥98%(HPLC)

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包装规格：10mg 50mg 100mg 250mg in glass bottle
溶解性：溶水DMSO(10mg/mL)。
产品描述：基本信息 产品编号：H10051 产品名称：H-89 CAS: 127243-85-0   储存条件 粉末 -20℃ 四年 分子式： C20H20BrN3O2S 溶于液体 -80℃ 两年 分子量 446.36     化学名：      Solubility (25°C)   体外 DMSO 100mg/mL (192.57mM) Ethanol 4mg/mL (7.7mM) Water Insoluble 体内（现配现用）     ＜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 1.9257mL 9.6287mL 19.2574mL 5mM 0.3851mL 1.9257mL 3.8515mL 10mM 0.1926mL 0.9629mL 1.9257mL 50mM 0.0385mL 0.1926mL 0.3851mL   生物活性 产品描述 一种DDA抑制剂。 靶点/IC50 PKA(Cell-free assay) S6K1(Cell-free assay) PKG(Cell-free assay) 48nM(Ki) 80nM 0.48μM(Ki) 体外研究 H-89 inhibits protein kinase A, in competitive fashion against ATP. H-89 causes a dose-dependent inhibition of the forskolininduced protein phosphorylation, with no decrease in intracellular cyclic AMP levels in PC12D cells. H-89 significantly inhibits the forskolin-induced neurite outgrowth from PC12D cells. H-89 (30μM) inhibits significantly cAMP-dependent histone IIb phosphorylation activity in PC12D cell lysates. H-89 (1-2μM) significantly slows the repriming rate in rat skinned fibres, most likely due to it deleteriously affecting the T-system potential. H-89 (10-100μM) inhibits net Ca2+ uptake by the SR and affectes the Ca32-sensitivity of the contractile apparatus in rat skinned fibres. 体内研究 H-89 (0.2mg/100g, i.p.) significantly increases seizure latency and threshold in PTZ-treated animals. H-89 (0.05, 0.2mg/100g, i.p.) prevents the epileptogenic activity of bucladesine (300nM)with significant increase of seizure latency and seizure threshold.   推荐实验方法(仅供参考) 激酶实验： Kinase activities are assayed at 30℃ for 2-5 min by measuring the transfer of 32P from [γ-32P]ATP to substrates. The reaction is terminated by adding 1mL of 20% trichloroacetic acid, following the addition of 100μg of bovine serum albumin as a carrier protein. The sample is centrifuged at 3000 rpm for 10 min, the pellet is resuspended in 5% trichloroacetic acid solution, the final pellet is dissolved in 1mL of 1N NaOH and the radioactivity is measured in a liquid scintillation counter.   细胞实验:   After 48 h in culture, PCl2D cells are cultured in test medium containing 30μM H-89 for 1h and then exposed to fresh medium that contained both 10μM forskolin and 30μM H-89. Cells are scraped off with a rubber policeman and sonicated in the presence of 0.5mL of 6% trichloroacetic acid. To extract trichloroacetic acid, 2mL of petroleum ether is added, the preparation mixed and centrifuged at 3000 rpm for 10 min. After aspiration of the upper layer, the residue sample solution is used for determination.   动物实验:   Male albino mice weighing 20-25 g are obtained. Pentoxifylline (25, 50, 100mg/kg), bucladesine (50, 100, 300nM/mouse)and H-89 (0.05, 0.1, 0.2mg/100g) are administered intraperitoneally (i.p.) 30 min before intravenous (i.v.) infusion of PTZ. In combination groups, the first and second components are injected 45 and 30 min before PTZ infusion. In all groups, the respective control animalsreceive an appropriate volume of vehicle. For the i.v. infusion, the needle is inserted into the lateral tail vein, fixed to the tail vein by a narrow piece of adhesive tape, and the animal is allowed to move freely. PTZ solution is infused at a concentration rate of 1mL/min.
保存条件：-20℃

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