H-89 dihydrochloride hydrate - CAS:130964-39-5 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	H-89 dihydrochloride hydrate 促销
英文名称:	H-89 dihydrochloride hydrate
别名:	N-[2-(p-Bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide dihydrochloride
CAS No:	130964-39-5	分子式:	C₂₀H₂₀BrN₃O₂S^.₂HCl^.XH₂O	分子量:	519.28
CAS No:	130964-39-5
分子式:	C₂₀H₂₀BrN₃O₂S^.₂HCl^.XH₂O
分子量:	519.28
MDL:	MFCD11045926

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H10026 H-89 dihydrochloride hydrate ≥98%(HPLC) (psaitong)

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熔点：

141-143°C

包装规格：

5mg 25mg 100mg in glass bottle

溶解性：

溶于DMSO(100 mg/ml)

产品描述：

基本信息

产品编号：H10026
产品名称：H-89 dihydrochloride hydrate
CAS:	130964-39-5	储存条件	粉末	2-8℃	四年

分子式：	C20H20BrN3O2S.2HCl.XH2O		溶于液体	-80℃	六个月
分子量	519.28			-20℃	一个月
化学名：
Solubility (25°C)	体外	DMSO
		Ethanol
		Water
	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

生物活性

产品描述	一种强效的细胞渗透性和可逆的protein kinase A(PKA)抑制剂。
靶点/IC₅₀	PKA (Cell-free assay)	S6K1 (Cell-free assay)	PKG (Cell-free assay)	PKA (Cell-free assay)
靶点/IC₅₀	48nM(Ki)	80nM	0.48μM(Ki)	48nM(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 Ca2+-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：
PKA酶活性	cAMP依赖性蛋白激酶活性在反应混合物中测定，反应混合物终体积为0.2mL，包含50mM Tris-HC1 (pH 7.0)，10mM 醋酸镁，2mM EGTA，1μM cAMP 或不加cAMP，3.3-20μM [γ-32P]ATP (4 × 105 cpm)，0.5μg 酶，100 μg组蛋白H2B，以及如上所述的所有化合物。

细胞实验:

After 48h in culture, PCl2D cells are cultured in test medium containing 30μM H-89 for 1 h 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 10min. After aspiration of the upper layer, the residue sample solution is used for determination.

动物实验:

Male albino mice weighing 20-25g are obtained. BL-191 (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：

2-8℃

UN码：

HazardClass：

危害声明：

安全说明：

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