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是一种有效的 ROCK1,PKA,PKC 和 MLCK 抑制剂,Ki 值分别为 0.33 μM,1.0 μM,9.3 μM 和 55 μM。",{"key":254,"value":255},"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":257,"value":258},"靶点","p160ROCK:0.33 μM (Ki)\nPKA:1 μM (Ki)\nPKC:9.3 μM (Ki)\nMLCK:55 μM (Ki)",{"key":260,"value":261},"体外研究","法舒地尔盐酸盐具有血管舒张作用,并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":263,"value":264},"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":266,"value":267},"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测量放射性。",{"key":269,"value":270},"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. Nature. 1997 Oct 30;389(6654):990-4.",[],[],[274,277,280,283],{"key":275,"value":276},"海关编码","2933990090",{"key":278,"value":279},"中文概述","2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%",{"key":281,"value":282},"申报要素","品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期",{"key":284,"value":285},"Summary","2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%",[287,290,293,296],{"key":288,"value":289},"危害码 (欧洲)","Xi",{"key":291,"value":292},"WGK德国","3",{"key":294,"value":295},"RTECS号","HM4031166",{"key":275,"value":297},"2942000000","\u003Ctd>\n\n\u003Cp>\u003Ca href=\"\u002Fen\u002Fcas\u002F105628-07-7_1029964.html#duXinDiv\">盐酸法舒地尔毒性英文版\u003C\u002Fa>\u003C\u002Fp>\n\n\u003C\u002Ftd>","\u003Ctd>\n\r\n                                        \r\n                                        盐酸法舒地尔\n\u003Cb>修改号码：4\u003C\u002Fb>\n\u003Cbr \u002F>\n\n\u003Cstrong>模块1. 化学品\u003C\u002Fstrong>\n\u003Cbr \u002F> 产品名称：\n\u003Cb>Fasudil Hydrochloride\u003C\u002Fb>\n\u003Cbr \u002F> 修改号码：\n\u003Cb>4\u003C\u002Fb>\n\u003Cbr \u002F>\n\n\u003Cstrong>模块2. 危险性概述\u003C\u002Fstrong>\n\u003Cbr \u002F>\n\u003Cb>GHS分类\u003C\u002Fb>\n\u003Cbr \u002F> 　物理性危害未分类\n\u003Cbr \u002F> 　健康危害\n\u003Cbr \u002F> 急性毒性（经口）\n\u003Cb>第4级\u003C\u002Fb>\n\u003Cbr \u002F> 　环境危害未分类\n\u003Cbr \u002F>\n\u003Cb>GHS标签元素\u003C\u002Fb>\n\u003Cbr \u002F> 　图标或危害标志\n\u003Cbr \u002F> 　信号词警告\n\u003Cbr \u002F> 　危险描述吞咽有害。\n\u003Cbr \u002F> 　防范说明\n\u003Cbr \u002F>\n\u003Cb>[预防]\u003C\u002Fb>使用本产品时切勿吃东西，喝水或吸烟。\n\u003Cbr \u002F> 处理后要彻底清洗双手。\n\u003Cbr \u002F>\n\u003Cb>[急救措施]\u003C\u002Fb>\n\u003Cb>食入：若感不适，呼叫解毒中心\u002F医生。漱口。\u003C\u002Fb>\n\u003Cbr \u002F>\n\u003Cb>[废弃处置]\u003C\u002Fb>\n\u003Cb>根据当地政府规定把物品\u002F容器交与工业废弃处理机构。\u003C\u002Fb>\n\u003Cbr \u002F>\n\n\u003Cstrong>模块3. 成分\u002F组成信息\u003C\u002Fstrong>\n\u003Cbr \u002F>\n\u003Cb>单一物质\u002F混和物\u003C\u002Fb>单一物质\n\u003Cbr \u002F>\n\u003Cb>化学名(中文名)：\u003C\u002Fb>盐酸法舒地尔\n\u003Cbr \u002F> 百分比：\n\u003Cb>&gt;98.0%(LC)\u003C\u002Fb>\n\u003Cbr \u002F>\n\u003Cb>CAS编码：\u003C\u002Fb>\n\u003Cb>105628-07-7\u003C\u002Fb>\n\u003Cbr \u002F> 俗名：\n\u003Cb>1-(5-Isoquinolinesulfonyl)homopiperazine Hydrochloride , 5-(1-\u003C\u002Fb>\n\u003Cbr \u002F>\n\u003Cb>Homopiperazinyl)sulfonylisoquinoline Hydrochloride\u003C\u002Fb>\n\u003Cbr \u002F> 分子式：\n\u003Cb>C14H17N3O2S·HCl\u003C\u002Fb>\n\u003Cbr \u002F>\n\n\u003Cstrong>模块4. 急救措施\u003C\u002Fstrong>\n\u003Cbr \u002F> 吸入：\n\u003Cb>将受害者移到新鲜空气处，保持呼吸通畅，休息。若感不适请求医\u002F就诊。\u003C\u002Fb>\n\u003Cbr \u002F> 盐酸法舒地尔\n\u003Cb>修改号码：4\u003C\u002Fb>\n\u003Cbr \u002F>\n\n\u003Cstrong>模块4. 急救措施\u003C\u002Fstrong>\n\u003Cbr \u002F> 皮肤接触：\n\u003Cb>立即去除\u002F脱掉所有被污染的衣物。用水清洗皮肤\u002F淋浴。\u003C\u002Fb>\n\u003Cbr \u002F>\n\u003Cb>若皮肤刺激或发生皮疹：求医\u002F就诊。\u003C\u002Fb>\n\u003Cbr \u002F> 眼睛接触：用水小心清洗几分钟。如果方便，易操作，摘除隐形眼镜。继续清洗。\n\u003Cbr \u002F>\n\u003Cb>如果眼睛刺激：求医\u002F就诊。\u003C\u002Fb>\n\u003Cbr \u002F> 食入：\n\u003Cb>若感不适，呼叫解毒中心\u002F医生。漱口。\u003C\u002Fb>\n\u003Cbr \u002F> 紧急救助者的防护：救援者需要穿戴个人防护用品，比如橡胶手套和气密性护目镜。\n\u003Cbr \u002F>\n\n\u003Cstrong>模块5. 消防措施\u003C\u002Fstrong>\n\u003Cbr \u002F> 合适的灭火剂：干粉，泡沫，雾状水，二氧化碳\n\u003Cbr \u002F> 特殊危险性：小心，燃烧或高温下可能分解产生毒烟。\n\u003Cbr \u002F> 特定方法：从上风处灭火，根据周围环境选择合适的灭火方法。\n\u003Cbr \u002F> 非相关人员应该撤离至安全地方。\n\u003Cbr \u002F> 周围一旦着火：如果安全，移去可移动容器。\n\u003Cbr \u002F> 消防员的特殊防护用具：灭火时，一定要穿戴个人防护用品。\n\u003Cbr \u002F>\n\n\u003Cstrong>模块6. 泄漏应急处理\u003C\u002Fstrong>\n\u003Cbr \u002F> 个人防护措施，防护用具，\n\u003Cb>使用个人防护用品。远离溢出物\u002F泄露处并处在上风处。\u003C\u002Fb>\n\u003Cbr \u002F> 紧急措施：泄露区应该用安全带等圈起来，控制非相关人员进入。\n\u003Cbr \u002F> 环保措施：防止进入下水道。\n\u003Cbr \u002F> 控制和清洗的方法和材料：清扫收集粉尘，封入密闭容器。注意切勿分散。附着物或收集物应该立即根据合适的\n\u003Cbr \u002F> 法律法规处置。\n\u003Cbr \u002F>\n\n\u003Cstrong>模块7. 操作处置与储存\u003C\u002Fstrong>\n\u003Cbr \u002F> 处理\n\u003Cbr \u002F> 技术措施：在通风良好处进行处理。穿戴合适的防护用具。防止粉尘扩散。处理后彻底清洗双手\n\u003Cbr \u002F> 和脸。\n\u003Cbr \u002F> 注意事项：如果粉尘或浮质产生，使用局部排气。\n\u003Cbr \u002F> 操作处置注意事项：避免接触皮肤、眼睛和衣物。\n\u003Cbr \u002F> 贮存\n\u003Cbr \u002F> 储存条件：保持容器密闭。存放于凉爽、阴暗处。\n\u003Cbr \u002F> 远离不相容的材料比如氧化剂存放。\n\u003Cbr \u002F> 包装材料：依据法律。\n\u003Cbr \u002F>\n\n\u003Cstrong>模块8. 接触控制和个体防护\u003C\u002Fstrong>\n\u003Cbr \u002F> 工程控制：尽可能安装封闭体系或局部排风系统，操作人员切勿直接接触。同时安装淋浴器和洗\n\u003Cbr \u002F> 眼器。\n\u003Cbr \u002F> 个人防护用品\n\u003Cbr \u002F> 　呼吸系统防护：防尘面具。依据当地和政府法规。\n\u003Cbr \u002F> 　手部防护：防护手套。\n\u003Cbr \u002F> 　眼睛防护：安全防护镜。如果情况需要，佩戴面具。\n\u003Cbr \u002F> 　皮肤和身体防护：防护服。如果情况需要，穿戴防护靴。\n\u003Cbr \u002F>\n\n\u003Cstrong>模块9. 理化特性\u003C\u002Fstrong>\n\u003Cbr \u002F> 固体\n\u003Cbr \u002F>\n\u003Cb>外形（20°C）：\u003C\u002Fb>\n\u003Cbr \u002F> 外观：\n\u003Cb>晶体-粉末\u003C\u002Fb>\n\u003Cbr \u002F> 颜色：白色类白色\n\u003Cbr \u002F> 气味：无资料\n\u003Cbr \u002F>\n\u003Cb>pH:\u003C\u002Fb>无数据资料\n\u003Cbr \u002F> 熔点：\n\u003Cb>222°C (分解)\u003C\u002Fb>\n\u003Cbr \u002F> 盐酸法舒地尔\n\u003Cb>修改号码：4\u003C\u002Fb>\n\u003Cbr \u002F>\n\n\u003Cstrong>模块9. 理化特性\u003C\u002Fstrong>\n\u003Cbr \u002F>\n\u003Cb>沸点\u002F沸程\u003C\u002Fb>无资料\n\u003Cbr \u002F> 闪点：无资料\n\u003Cbr \u002F> 爆炸特性\n\u003Cbr \u002F> 　爆炸下限：无资料\n\u003Cbr \u002F> 　爆炸上限：无资料\n\u003Cbr \u002F> 密度：无资料\n\u003Cbr \u002F> 溶解度：溶于： 水 甲醇\n\u003Cbr \u002F> 极微溶于： 乙醇\n\u003Cbr \u002F> 不溶于： 醚\n\u003Cbr \u002F>\n\n\u003Cstrong>模块10. 稳定性和反应性\u003C\u002Fstrong>\n\u003Cbr \u002F> 化学稳定性：一般情况下稳定。\n\u003Cbr \u002F> 危险反应的可能性：未报道特殊反应性。\n\u003Cbr \u002F> 须避免接触的物质氧化剂\n\u003Cbr \u002F>\n\u003Cb>危险的分解产物:\u003C\u002Fb>\n\u003Cb>一氧化碳, 二氧化碳, 氮氧化物 (NOx), 硫氧化物, 氯化氢\u003C\u002Fb>\n\u003Cbr \u002F>\n\n\u003Cstrong>模块11. 毒理学信息\u003C\u002Fstrong>\n\u003Cbr \u002F> 急性毒性：\n\u003Cb>orl-rat LD50:335 mg\u002Fkg\u003C\u002Fb>\n\u003Cbr \u002F>\n\u003Cb>scu-rat LD50:123 mg\u002Fkg\u003C\u002Fb>\n\u003Cbr \u002F>\n\u003Cb>ivn-rat LD50:59900 ug\u002Fkg\u003C\u002Fb>\n\u003Cbr \u002F> 对皮肤腐蚀或刺激：无资料\n\u003Cbr \u002F> 对眼睛严重损害或刺激：无资料\n\u003Cbr \u002F> 生殖细胞变异原性：无资料\n\u003Cbr \u002F> 致癌性：\n\u003Cbr \u002F>\n\u003Cb>IARC =\u003C\u002Fb>无资料\n\u003Cbr \u002F>\n\u003Cb>NTP =\u003C\u002Fb>无资料\n\u003Cbr \u002F> 生殖毒性：无资料\n\u003Cbr \u002F>\n\u003Cb>RTECS 号码:\u003C\u002Fb>\n\u003Cb>HM4033500\u003C\u002Fb>\n\u003Cbr \u002F>\n\n\u003Cstrong>模块12. 生态学信息\u003C\u002Fstrong>\n\u003Cbr \u002F> 生态毒性：\n\u003Cbr \u002F> 鱼类：无资料\n\u003Cbr \u002F> 甲壳类：无资料\n\u003Cbr \u002F> 藻类：无资料\n\u003Cbr \u002F>\n\u003Cb>残留性 \u002F 降解性：\u003C\u002Fb>无资料\n\u003Cbr \u002F>\n\u003Cb>潜在生物累积 （BCF):\u003C\u002Fb>无资料\n\u003Cbr \u002F> 土壤中移动性\n\u003Cbr \u002F>\n\u003Cb>　log水分配系数：\u003C\u002Fb>无资料\n\u003Cbr \u002F>\n\u003Cb>　土壤吸收系数 （Koc）：\u003C\u002Fb>无资料\n\u003Cbr \u002F> 　亨利定律无资料\n\u003Cbr \u002F>\n\u003Cb>constant(PaM3\u002Fmol):\u003C\u002Fb>\n\u003Cbr \u002F>\n\n\u003Cstrong>模块13. 废弃处置\u003C\u002Fstrong>\n\u003Cbr \u002F> 如果可能，回收处理。请咨询当地管理部门。建议在可燃溶剂中溶解混合，在装有后燃和洗涤装置的化学焚烧炉中\n\u003Cbr \u002F> 焚烧。废弃处置时请遵守国家、地区和当地的所有法规。\n\u003Cbr \u002F>\n\n\u003Cstrong>模块14. 运输信息\u003C\u002Fstrong>\n\u003Cbr \u002F> 联合国分类：与联合国分类标准不一致\n\u003Cbr \u002F>\n\u003Cb>UN编号：\u003C\u002Fb>未列明\n\u003Cbr \u002F> 盐酸法舒地尔\n\u003Cb>修改号码：4\u003C\u002Fb>\n\u003Cbr \u002F>\n\n\u003Cstrong>模块15. 法规信息\u003C\u002Fstrong>\n\u003Cbr \u002F>\n\u003Cb>《危险化学品安全管理条例》（2002年1月26日国务院发布，2011年2月16日修订）: 针对危险化学品的安全使用、\u003C\u002Fb>\n\u003Cbr \u002F> 生产、储存、运输、装卸等方面均作了相应的规定。\n\u003Cbr \u002F>\n\u003Cbr \u002F>\n\n\u003Cstrong> 模块16 - 其他信息 \u003C\u002Fstrong>\n\u003Cbr \u002F>N\u002FA\n\u003Cbr \u002F>\n\u003Cbr \u002F>\u003Cbr \u002F>\u003Cbr \u002F>\n\u003C\u002Ftd>","2026-11-04T01:18:52.274175Z",false,[303,309,315,321,327,333,339,345,351,357,363,369],{"slug":304,"cid":305,"name":306,"nameZh":307,"cas":308},"785905339009601536","J-172626-7","Benzyl 11-aminoundecanoate hydrochloride","11-氨基十一烷酸苄酯盐酸盐","101778-85-2",{"slug":310,"cid":311,"name":312,"nameZh":313,"cas":314},"855016484450078720","J-1994354-5","ABS-752 (hydrochloride)","ABS-752 盐酸盐","2922884-90-8",{"slug":316,"cid":317,"name":318,"nameZh":319,"cas":320},"785881811828871168","J-21152-9","Methyl perfluorohexanoate","十一氟己酸甲酯","424-18-0",{"slug":322,"cid":323,"name":324,"nameZh":325,"cas":326},"785893664441241600","J-35896-3","Retinyl acetate","维生素A醋酸酯","127-47-9",{"slug":328,"cid":329,"name":330,"nameZh":331,"cas":332},"785871921307717632","J-1990316-3","Tetraamminepalladium(II) acetate","四氨基醋酸钯","61495-96-3",{"slug":334,"cid":335,"name":336,"nameZh":337,"cas":338},"785872502957019136","J-1992231-7","Europium(III) acetate hydrate","乙酸铕水合物","62667-64-5",{"slug":340,"cid":341,"name":342,"nameZh":343,"cas":344},"785883812713205760","J-1174874-6","Calcium valproate","丙戊酸钙","33433-82-8",{"slug":346,"cid":347,"name":348,"nameZh":349,"cas":350},"785889759493885952","J-1378692-0","Calcium 2-ethylhexanoate","2-乙基己酸钙","136-51-6",{"slug":352,"cid":353,"name":354,"nameZh":355,"cas":356},"785891472418279424","J-1306502-6","calcium caprylate","辛酸钙","6107-56-8",{"slug":358,"cid":359,"name":360,"nameZh":361,"cas":362},"785891472565080064","J-1348387-9","Calcium isooctanoate","异辛酸钙","84777-61-7",{"slug":364,"cid":365,"name":366,"nameZh":367,"cas":368},"785898943622942720","J-1322115-3","Cerium citrate","柠檬酸铈","512-24-3",{"slug":370,"cid":371,"name":372,"nameZh":373,"cas":374},"785883944527597568","J-41268-0","Fumaric acid monoethyl ester, calcium salt","富马酸单乙基酯钙盐","62008-22-4",1794261709536,"zh-CN",[378],{"slug":234,"name":233,"nameZh":232,"origin":30,"originFlag":31}]