中文名 | 法舒地尔 |
英文名 | Fasudil |
别名 | 法舒地尔 法舒地尔原料药 1-(5-硫代异喹啉)哌嗪二盐酸盐 六氢-1-(5-异喹啉基磺酰基)-1H-1,4-二氮卓 六氢-1-(5-异喹啉磺酰基)-1H-1,4-二氮杂卓 |
英文别名 | at877 Fasudil 103745-39-7 Fasudil HCI Fasudil Hydrchloride Fasudil Hydrochloride Injection (5-ISOQUINOLINESULFONYL)HOMOPIPERAZINE 1-(5-Isoquinolinesulphonyl)homopiperazine 5-(1,4-Diazepan-1-ylsulfonyl)isoquinoline 1-(5-Isoquinolinylsulfonyl)homopiperazine 1-(5-ISOQUINOLINE-SULFONYL)-HOMOPIPERAZINE 5-(1,4-diazepan-4-ium-1-ylsulfonyl)isoquinoline N-(5-Isoquinolinesulfonyl)-1,4-perhydrodiazepine 5-(AZEPAN-4-YLSULFONYL)ISOQUINOLINE DIHYDROCHLORIDE hexahydro-1-(5-isoquinolinylsulfonyl)-1h-4-diazepine 5-(1,4-diazepan-1-ylsulfonyl)isoquinoline dihydrochloride isoquinoline, 5-[(hexahydro-1H-1,4-diazepin-1-yl)sulfonyl]- |
CAS | 103745-39-7 |
EINECS | 816-154-4 |
化学式 | C14H17N3O2S |
分子量 | 291.37 |
InChI | InChI=1/C14H17N3O2S.2ClH/c18-20(19,17-9-2-6-15-8-10-17)14-4-1-3-12-11-16-7-5-13(12)14;;/h1,3-5,7,11,15H,2,6,8-10H2;2*1H |
密度 | 1.289±0.06 g/cm3(Predicted) |
沸点 | 506.2±60.0 °C(Predicted) |
闪点 | 284.9°C |
水溶性 | Soluble in water or DMSO |
蒸汽压 | 2.55E-12mmHg at 25°C |
溶解度 | H2O: >200mg/ml |
酸度系数 | 9.73±0.20(Predicted) |
存储条件 | Store at RT |
外观 | 固体 |
颜色 | white |
物化性质 | 盐酸法舒地尔(Fasudil Hydrochloride):C14H17N3O2S?HCl。[105628-07-7]。从水结晶,熔点220.5℃。白色结晶性粉末,熔点219.3℃。水中溶解度在Ph=5.0~7.0时可达2×10-2mol/L。急性毒性LD50小鼠,大鼠(mg/kg):67.5,59.9静脉注射;124.5,123.2皮下注射;273.9,335.0口服。 |
体内研究 | Fasudil (intravenous injection; 0.01, 0.03, 0.1 and 0.3 mg/kg) decreases MBP and increases HR, VBF, CBF, RBF, and FBF. Fasudil (1.0 ng/mL) increases cardiac output. Fasudil via i.v. produces a significant fall in MBP, left ventricular systolic pressure and total peripheral resistance with an increase in HR and cardiac output, but without obvious effect on right atrial pressure, dP/dt or left ventricular minute work in dogs. Fasudil exhibits protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury. Fasudil (orally administration; 100 mg/kg/day) significantly reduces incidence and mean maximum clinical score of EAE in SJL/J mice immunized with PLP p139-151. Fasudil inhibits the proliferative response of splenocytes to the antigen in mice. Fasudil decreases inflammation, demyelination, axonal loss and APP positivein spinal cord of Fasudil-treated mice via p.o. administration. |
WGK Germany | 3 |
RTECS | HM4031166 |
海关编号 | 29334900 |
上游原料 | 异喹啉 |
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