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127243-85-0

中文名称 H-89二盐酸盐
英文名称 N-(2-[P-BROMOCINNAMYLAMINO]ETHYL)-5-ISOQUINOLINESULFONAMIDE HYDROCHLORIDE
CAS 127243-85-0
分子式 C20H20BrN3O2S
MDL 编号 MFCD00214119
分子量 446.36
MOL 文件 127243-85-0.mol
更新日期 2024/04/22 14:25:56
127243-85-0 结构式 127243-85-0 结构式

基本信息

中文别名
H-89二盐酸盐
N-[2-[P-溴苯丙烯盐基氨基]乙基]-5-异喹啉磺酰胺
英文别名
H-89
H-89 DIHYDROCHLORIDE
H-89 HYDROCHLORIDE
N-[2-(P-BROMOCINNAMYLAMINO)ETHYL]-5-ISOQUINOLINE SULFONAMIDE
N-[2-(P-BROMOCINNAMYLAMINO)ETHYL]-5-ISOQUINOLINESULFONAMIDE 2HCL
N-[2-(P-BROMOCINNAMYLAMINO)ETHYL]-5-ISOQUINOLINE SULFONAMIDE, DIHYDROCHLORIDE
N-(2-[P-BROMOCINNAMYLAMINO]ETHYL)-5-ISOQUINOLINESULFONAMIDE HYDROCHLORIDE
N-[2-[P-BROMOCINNAMYLAMINO]-ETHYL]-5-ISOQUINOLINESULFONMIDE
所属类别
生物化工:激动剂抑制剂

物理化学性质

熔点195-200°C
沸点639.7±65.0 °C(Predicted)
密度1.436
储存条件2-8°C
溶解度H2O: ≥10 mg/mL
酸度系数(pKa)10.43±0.50(Predicted)
形态powder
形态粉末
颜色off-white
颜色米白色
稳定性Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months.

知名试剂公司产品信息

常见问题列表

生物活性
H-89 是一种有效、选择性的 cAMP 依赖性 protein kinase A 抑制剂,IC50 值为 48 nM,对 PKG,PKC,Casein Kinase 和其他激酶的抑制作用很弱。
靶点

IC50: 48 nM (protein kinase A)

体外研究

H-89 inhibits protein kinase A, in competitive fashion against ATP. H-89 causes a dose-dependent inhibition of the forskolin-induced 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 (30 μM) inhibits significantly cAMP-dependent histone IIb phosphorylation activity in PC12D cell lysates. H-89 (1-2 μM) significantly slows the repriming rate in rat skinned fibres, most likely due to it deleteriously affecting the T-system potential. H-89 (10-100 μM) inhibits net Ca 2+ uptake by the SR and affectes the Ca 32 -sensitivity of the contractile apparatus in rat skinned fibres.

体内研究

H-89 (0.2 mg/100g, i.p.) significantly increases seizure latency and threshold in PTZ-treated animals. H-89 (0.05, 0.2 mg/100 g, i.p.) prevents the epileptogenic activity of bucladesine (300 nM) with significant increase of seizure latency and seizure threshold.

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