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Da\n8、标称质量：363 Da\n9、平均质量：364.2906 Da",{"label":237,"labelZh":238,"value":239},"Computational Chemistry","计算化学","1、 疏水参数计算参考值（XlogP）：1\n2、 氢键供体数量：1\n3、 氢键受体数量：5\n4、 可旋转化学键数量：2\n5、 互变异构体数量：\n6、 拓扑分子极性表面积（TPSA）：62.3\n7、 重原子数量：20\n8、 表面电荷：0\n9、 复杂度：421\n10、同位素原子数量：0\n11、确定原子立构中心数量：0\n12、不确定原子立构中心数量：0\n13、确定化学键立构中心数量：0\n14、不确定化学键立构中心数量：0\n15、共价键单元数量：1",{"label":229,"labelZh":241,"value":242},"更多","1. 性状：白色粉末\n2. 密度（g\u002FmL,25℃）：未确定\n3. 相对蒸汽密度（g\u002FmL,空气=1）：未确定\n4. 熔点（ºC）：219.3\n5. 沸点（ºC,常压）：未确定\n6. 沸点（ºC，0.04mmHg）：未确定\n7. 折射率(n20\u002FD)：未确定\n8. 闪点（ºC）：未确定\n9. 比旋光度（º）：未确定\n10. 自燃点或引燃温度（ºC）：未确定\n11. 蒸气压（mmHg,20ºC）：未确定\n12. 饱和蒸气压（kPa,25ºC）：未确定\n13. 燃烧热（KJ\u002Fmol）：未确定\n14. 临界温度（ºC）：未确定\n15. 临界压力（KPa）：未确定\n16. 油水（辛醇\u002F水）分配系数的对数值：未确定\n17. 爆炸上限（%,V\u002FV）：未确定\n18. 爆炸下限（%,V\u002FV）：未确定\n19. 溶解性：溶于水",null,[],[246,249,252,255,258,261,264],{"key":247,"value":248},"描述","Fasudil 是一种有效的 ROCK1,PKA,PKC 和 MLCK 的抑制剂,Ki 值分别为 0.33 μM,1.0 μM,9.3 μM 和 55 μM。",{"key":250,"value":251},"相关类别","信号通路\n>>\n自噬\n>>\n自噬\n信号通路\n>>\n蛋白酪氨酸激酶\n>>\nPKA\n信号通路\n>>\n干细胞及 Wnt 通路\n>>\nPKA\n信号通路\n>>\n细胞周期\u002FDNA损伤\n>>\n岩石\n信号通路\n>>\n干细胞及 Wnt 通路\n>>\n岩石\n信号通路\n>>\nTGF-beta\u002FSmad 信号通路\n>>\n岩石\n研究领域\n>>\n癌症",{"key":253,"value":254},"靶点","p160ROCK:0.33 μM (Ki)\nPKA:1 μM (Ki)\nPKC:9.3 μM (Ki)\nMLCK:55 μM (Ki)",{"key":256,"value":257},"体外研究","法舒地尔具有血管扩张作用,占据酶结合位点的腺嘌呤口袋[1]。法舒地尔对去极化兔主动脉的Ca2 +诱导的收缩产生竞争性抑制作用。法舒地尔抑制对KCl,苯乙烯(PHE)和前列腺素(PG)F2a的收缩反应[2]。法舒地尔还通过抑制5-羟色胺,去甲肾上腺素,组胺,血管紧张素和多巴胺诱导的螺旋条收缩而表现出血管舒张作用[3]。此外,法舒地尔诱导肌动蛋白应力纤维的解体和细胞迁移抑制[4]。法舒地尔抑制肝星状细胞扩散,应激纤维的形成和α-SMA的表达,同时抑制细胞生长,但不诱导细胞凋亡。法舒地尔还阻断了LPA诱导的ERK1\u002F2,JNK和p38 MAPK的磷酸化[5]。",{"key":259,"value":260},"体内研究","法舒地尔(30μg)通过冠状动脉内注射给狗增加了50％的CBF。法舒地尔(0.01,0.03,0.1和0.3 mg\u002Fkg,推注,静脉注射)可降低MBP并增加HR,VBF,CBF,RBF和FBF。法舒地尔(1.0 ng\u002FmL)可增加心输出量。法舒地尔通过静脉注射导致MBP,左心室收缩压和总外周阻力显着下降,HR和心输出量增加,但对右心房压,dP\u002Fdt或左心室分钟工作没有明显影响[3]。法舒地尔对心血管疾病具有可保护作用,减少JNK的激活,减轻缺血性损伤后AIF的线粒体-核转位[6]。法舒地尔(100mg\u002Fkg \u002F天,口服)显着降低用PLP p139-151免疫的SJL\u002FJ小鼠的EAE的发生率和平均最大临床评分。法舒地尔抑制脾细胞对小鼠抗原的增殖反应。法舒地尔通过口服给药减少法舒地尔治疗小鼠的炎症,脱髓鞘,轴突缺失和脊髓APP阳性[7]。",{"key":262,"value":263},"激酶实验","在含有最终体积0.2mL，50mM Tris-HCl（pH 7.0），10mM乙酸镁，2mM EGTA，1μM环AMP或不含环状的反应混合物中测定环AMP依赖性蛋白激酶活性。 AMP，3.3至20μM[r-32P] ATP（4×105cpm），0.5μg酶，100μg组蛋白H2B和化合物。将混合物在30℃下孵育5分钟。加入500μg牛血清白蛋白作为载体蛋白后，加入1mL冰冷的20％三氯乙酸终止反应。将样品以3000rpm离心15分钟，将沉淀重悬于冰冷的10％三氯乙酸溶液中，并将离心 - 再悬浮循环重复三次。将最终的沉淀溶解在1mL的1N NaOH中，并用液体闪烁计数器[1]测量放射性。",{"key":265,"value":266},"参考文献","[1].\nOno-Saito N, et al. H-series protein kinase inhibitors and potential clinical applications. Pharmacol Ther. 1999 May-Jun;82(2-3):123-31.\n[2].\nAsano T, et al. Mechanism of action of a novel antivasospasm drug, HA1077. J Pharmacol Exp Ther. 1987 Jun;241(3):1033-40.\n[3].\nAsano T, et al. Vasodilator actions of HA1077 in vitro and in vivo putatively mediated by the inhibition of protein kinase. Br J Pharmacol. 1989 Dec;98(4):1091-100.\n[4].\nNegoro N, et al. The kinase inhibitor fasudil (HA-1077) reduces intimal hyperplasia through inhibiting migration and enhancing cell loss of vascular smooth muscle cells. Biochem Biophys Res Commun. 1999 Aug 19;262(1):211-5.\n[5].\nFukushima M, et al. Fasudil hydrochloride hydrate, a Rho-kinase (ROCK) inhibitor, suppresses collagen production and enhances collagenase activity in hepatic stellate cells. Liver Int. 2005 Aug;25(4):829-38.\n[6].\nZhang J, et al. Inhibition of the activity of Rho-kinase reduces cardiomyocyte apoptosis in heart ischemia\u002Freperfusion via suppressing JNK-mediated AIF translocation. Clin Chim Acta. 2009 Mar;401(1-2):76-80.\n[7].\nSun X, et al. The selective Rho-kinase inhibitor Fasudil is protective and therapeutic in experimental autoimmune encephalomyelitis. J Neuroimmunol. 2006 Nov;180(1-2):126-34.\n[8].\nUehata M, et al. Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension. 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General tariff:20.0%",[307,310,313],{"key":308,"value":309},"WGK德国","3",{"key":311,"value":312},"RTECS号","HM4031166",{"key":295,"value":296},"\u003Ctd>\n\n\u003Cp>\u003Cstrong>法舒地尔毒理学数据:\u003C\u002Fstrong>\u003C\u002Fp>\n\u003Cp>\u003C\u002Fp>\u003Cp>1、急性毒性：大鼠经静脉LD50：59.9mg\u002Fkg；小鼠经静脉LD50：67.5mg\u002Fkg；大鼠经皮下LD50：123.2mg\u002Fkg；小鼠经皮下LD50：124.5mg\u002Fkg；大鼠经口LD50：335.0mg\u002Fkg；小鼠经口LD50：273.9mg\u002Fkg；\u003C\u002Fp>\n\u003Cp>\u003C\u002Fp>\n\u003Cp>\u003Ca href=\"\u002Fen\u002Fcas\u002F103745-39-7_81075.html#duXinDiv\">法舒地尔毒性英文版\u003C\u002Fa>\u003C\u002Fp>\n\n\u003C\u002Ftd>","\u003Cp> 异喹啉经发烟硫酸磺化，生成的磺酸转化为磺酰氯，再和二氮革反应，得到产物。 \u003C\u002Fp>","2026-08-21T07:03:54.610157Z",false,[319,325,331,337,343,349],{"slug":320,"cid":321,"name":322,"nameZh":323,"cas":324},"785882572998578176","J-1361907-7","Methyl Red sodium salt","甲基红钠盐","845-10-3",{"slug":326,"cid":327,"name":328,"nameZh":329,"cas":330},"785897942564212736","J-1098773-5","Giemsa stain","吉氏色素","51811-82-6",{"slug":332,"cid":333,"name":334,"nameZh":335,"cas":336},"785883770937937920","J-1394584-4","Calcium ferrocyanide","亚铁氰化钙","13821-08-4",{"slug":338,"cid":339,"name":340,"nameZh":341,"cas":342},"785898319372095488","J-1987692-2","Sodium starch glycolate","羧甲基淀粉钠","9063-38-1",{"slug":344,"cid":345,"name":346,"nameZh":347,"cas":348},"785883839846158336","J-9665-6","propineb","丙森锌","12071-83-9",{"slug":350,"cid":351,"name":352,"nameZh":353,"cas":354},"785892791585607680","J-1099303-5","Paclobutrazol","多效唑","76738-62-0",1792645224275,"zh-CN",[]]