Y-27632dihydrochlorideisanATP-competitiveinhibitorofROCK-IandROCK-II,withK_iof220nMand300nMforROCK-IandROCK-II,respectively.

Ki:220/300nM(ROCK-I/II)^[1]

Y-27632inhibitstheROCKfamilyofkinases100timesmorepotentlythanotherkinasesincludingproteinkinaseC,cAMP-dependentkinaseandmyosinlightchainkinase.Y-27632prolongsthelagtimeanddelaystheappearanceofBrdU-labeledcellsinaconcentration-dependentmanner,delaysofabout1and4harenoticedintheSwiss3T3cellstreatedwith10and100μMY-27632,respectively^[1].Y-27632promotesneuronaldifferentiationofADIposetissue-derivedstemcells(ADSCs).Comparedto1.0and2.5μMY-27632inducedgroups,percentagesofneuroal-likecellsachievedapeakinthe5.0μMY-27632inducedgroup^[2].

Y-27632(5and10mg/kg)significantlyprolongstheonsettimeofmyoclonicjerkswhencomparewithsalinegroup.Y-27632(5and10mg/kg)significantlyprolongstheonsettimeofclonicconvulsionswhencomparewithsalinegroup^[3].TreatmentwithDimethylnitrosamine(DMN)causesasignificantdecreaseinratbodyandliverweight(DMN-Sgroup)comparedwithcontrolanimals(S-Sgroup).OralY27632(30mg/kg)essentiallypreventsthisDMN-inducedratbodyandliverweightloss(DMN-Ygroup)^[4].

• [1].IshizakiT,etal.PharmacologicalpropertiesofY-27632,aspecificinhibitorofrho-associatedkinases.MolPharmacol.2000May;57(5):976-83.

  [2].XueZW,etal.Rho-associatedcoiledkinaseinhibitorY-27632promotesneuronal-likedifferentiationofadulthumanadiposetissue-derivedstemcells.ChinMedJ(Engl).2012Sep;125(18):3332-5.

  [3].InanS,etal.AntiepilepticeffectsoftwoRho-kinaseinhibitors,Y-27632andfasudil,inmice.BrJPharmacol.2008Sep;155(1):44-51.

  [4].TadaS,etal.AselectiveROCKinhibitor,Y27632,preventsdimethylnitrosamine-inducedhepaticfibrosisinrats.JHepatol.2001Apr;34(4):529-36.

RecombinantROCK-I,ROCK-II,PKN,orcitronkinaseisexpressedinHeLacellsasMyc-taggedproteinsbytransfectionusingLipofectamine,andisprecipitatedfromthecelllysatesbytheuseof9E10monoclonalanti-MycantibodycoupledtoGprotein-Sepharose.Recoveredimmunocomplexesareincubatedwithvariousconcentrationsof[³²P]ATPand10mgofhistonetype2assubstratesintheabsenceorpresenceofvariousconcentrationsofeitherY-27632orY-30141at30°Cfor30mininatotalvolumeof30μLofthekinasebuffercontaining50mMHEPES-NaOH,pH7.4,10mMMgCl₂,5mMMnCl₂,0.02%Briji35,and2mMdithiothreitol.PKCaisincubatedwith5μM[³²P]ATPand200μg/mLhistonetype2assubstratesintheabsenceorpresenceofvariousconcentrationsofeitherY-27632orY-30141at30°Cfor10mininakinasebuffercontaining50mMTris-HCl,pH7.5,0.5mMCaCl2,5mMmagnesiumacetate,25μg/mLphosphatidylserine,50ng/mL12-O-tetradecanoylphorbol-13-acetateand0.001%leupeptininatotalvolumeof30μL.Incubationisterminatedbytheadditionof10μLof43Laemmlisamplebuffer.Afterboilingfor5min,themixtureissubjectedtoSDS-polyacrylamidegelelectrophoresisona16%gel.ThegelisstainedwithCoomassieBrilliantBlue,andthendried.Thebandscorrespondingtohistonetype2areexcised,andtheradioactivityismeasured^[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

Y-27632isdissolvedinwaterandstored^[1].

HeLacellsareplatedatadensityof3×10⁴cellsper3.5-cmdish.ThecellsareculturedinDMEMcontaining10%FBSinthepresenceof10mMThymidinefor16h.AfterthecellsarewashedwithDMEMcontaining10%FBS,theyareculturedforanadditional8h,andthen40ng/mLofNocodazoleisadded.After11.5hoftheNocodazoletreatment,variousconcentrationsofY-27632(0-300μM),Y-30141,orvehicleisaddedandthecellsareincubatedforanother30min^[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

Y-27632isdissolvedin0.9%NaCl(saline)(Mice)^[3].
Y-27632isdissolvedinsaline(finalconcentration2%)(Rat)^[4].

Mice^[3]
Male,inbredSwissalbinomice(2-3monthsold)weighing25-30gareused.Miceareinjectedwithasub-convulsivedoseofPTZ(35mg/kg,i.p.)(onMondays,WednesdaysandFridays)ofeachweekforatotalof11injections.AftereachPTZinjection,miceareobservedfor30minandtheoccurrenceofconvulsiveactivityisrecorded.After30min,themicearetheninjectedwitheitherFasudil(25mg/kg,i.p.)orY-27632(5mg/kg,i.p.)andreturnedtotheirhomecagesuntilthenextinjection.ControlmiceforFasudilandY-27632receivessaline.
Rat^[4]
MaleWistarKindArats(200-250g)areused.DMN(1g/mL)isdilutedtentimeswithsaline(finalconcentration1%)and10mg/kgperdayofDMNisinjectedintraperitoneally(i.p.)onthefirst3daysofeachweekfor4weeks.Y27632isgivenorallyonceperdayatadoseof30mg/kgfor4weeksstartingonthedayofthefirstinjectionofDMN.Thedoseof30mg/kgcorrectshypertensioninseveralratmodelswithouttoxicity.Twentyratsarerandomizedintofourexperimentalgroups(n=5ineachgroup)asfollows:(1)S-S(injectionofsalinei.p.andoraladministrationofsaline);(2)S-Y(injectionofsalinei.p.andoraladministrationofY27632);(3)DMN-S(DMNi.p.andoraladministrationofsaline);(4)DMN-Y(DMNi.p.andoraladministrationofY27632).Theratsareweighedeveryweek.Theyaresacrificedattheendofthefourthweekandtheliverisexcised.Inaddition,abloodsampleistakenimmediatelybeforetheratsaresacrificed.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

• [1].IshizakiT,etal.PharmacologicalpropertiesofY-27632,aspecificinhibitorofrho-associatedkinases.MolPharmacol.2000May;57(5):976-83.

  [2].XueZW,etal.Rho-associatedcoiledkinaseinhibitorY-27632promotesneuronal-likedifferentiationofadulthumanadiposetissue-derivedstemcells.ChinMedJ(Engl).2012Sep;125(18):3332-5.

  [3].InanS,etal.AntiepilepticeffectsoftwoRho-kinaseinhibitors,Y-27632andfasudil,inmice.BrJPharmacol.2008Sep;155(1):44-51.

  [4].TadaS,etal.AselectiveROCKinhibitor,Y27632,preventsdimethylnitrosamine-inducedhepaticfibrosisinrats.JHepatol.2001Apr;34(4):529-36.

320.26

C₁₄H₂₃Cl₂N₃O

129830-38-2

RoomtemperatureincontinentalUS;mayvaryelsewhere

DMSO:≥32mg/mL

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:98.53%

SelectBatch:HY-10583-21694HY-10583-21522HY-10583-21796

DataSheet(124KB)SDS(252KB)

COA(94KB)HNMR(168KB)RP-HPLC(184KB)LCMS(222KB)

HandlingInstructions(1252KB)

• [1].IshizakiT,etal.PharmacologicalpropertiesofY-27632,aspecificinhibitorofrho-associatedkinases.MolPharmacol.2000May;57(5):976-83.

  [2].XueZW,etal.Rho-associatedcoiledkinaseinhibitorY-27632promotesneuronal-likedifferentiationofadulthumanadiposetissue-derivedstemcells.ChinMedJ(Engl).2012Sep;125(18):3332-5.

  [3].InanS,etal.AntiepilepticeffectsoftwoRho-kinaseinhibitors,Y-27632andfasudil,inmice.BrJPharmacol.2008Sep;155(1):44-51.

  [4].TadaS,etal.AselectiveROCKinhibitor,Y27632,preventsdimethylnitrosamine-inducedhepaticfibrosisinrats.JHepatol.2001Apr;34(4):529-36.

品牌介绍

托烷司琼临床评价药物相关作用适应症托烷司琼CAS号:89565-68-4英文名称:Tropisetron英文同义词:icf205-930;TROPICACID;TROPISETRON;SS-TROPISETRON;BETA-TROPISETRON;Tropisetron(ICS205930);TROPISHTRONHYDROCHLORIDE;Indole-3-carbonylchloride;3-Tropanylindole-3-carboxylate;lαH，5Αh-Tropan-3α-ylindole-3-carboxylate中文名称:托烷司琼中文同义词:托普西隆;托普西龙;曲匹西龙;托烷司琼;Β-托烷司琼;CS-348;Β-内托烷司琼;吲哚-3-甲酰氯;Β-托烷司琼(光学异构体);Β-托烷司琼,托烷司琼异构体CBNumber:CB3236404分子式:C17H20N2O2分子量:284.35MOLFile:89565-68-4.mol化学性质安全信息用途供应商112化学性质安全信息用途供应商112托烷司琼化学性质熔点:201-202°C沸点:448.5±35.0°C(Predicted)密度:1.26储存条件:2-8°C溶解度:H2O:soluble形态:solid酸度系数(pKa):15.38±0.30(Predicted)颜色:whiteCAS数据库:Chemicalbook89565-68-4(CASDataBaseReference)安全信息WGKGermany:3托烷司琼化学药品说明书托烷司琼|药物应用信息托烷司琼性质、用途与生产工艺临床评价Sorbe等报道本品对含顺铂(剂量50～89mg/m2)化疗方案引起的急性呕吐完全控制率为63%。58例恶性肿瘤化疗所致恶心、呕吐者，应用托烷司琼或昂丹司琼8mg分别在同一病人前后2个化疗周期的第1d给药前30min静脉注射，并用地塞米松10mg静脉滴注。结果两药控制急性及迟发性恶心、呕吐的疗效基本相似，均可达81%～100%。本品对强致吐化疗药物顺铂的止吐疗效突出。药物相关作用饮食可略为延长本品的吸收。本品与利福平、苯巴比妥等肝酶诱导药同时使用，可加快代谢，故快代谢型者需增加剂量，慢者则不必。西咪替丁等肝酶抑制药对本品血药浓度无明显影响。适应症托烷司琼临床用于预防和治疗癌症化疗引起的恶心和呕吐。化学性质结晶，熔点201-202℃(二氯甲烷-乙酸乙酯)。单盐酸托烷司琼(TropisetronMonohydroehloride)：C17H20N2O2?HCI。[105826-92-4]。熔点283-285℃(分解)。用途有高效性和选择性的5-HT3受体拮抗剂。用于化疗所致的呕吐。用途为5-羟色胺拮抗药生产方法托品醇(I)和酰氯(Ⅱ)反应，可得托烷司琼。托烷司琼上下游产品信息上游原料托品醇下游产品

公司介绍

托烷司琼临床评价药物相关作用适应症托烷司琼CAS号:89565-68-4英文名称:Tropisetron英文同义词:icf205-930;TROPICACID;TROPISETRON;SS-TROPISETRON;BETA-TROPISETRON;Tropisetron(ICS205930);TROPISHTRONHYDROCHLORIDE;Indole-3-carbonylchloride;3-

品牌分类

黄酮类化合物 抑制性抗体 苯丙素类 酸和醛 醌类 肽 其他 酚类 萜类和糖苷类

类固醇 生物碱 糖类和糖苷类 染料试剂 生化分析试剂

显示分类

联络我们

服务热线：4000-520-616

（限工作日9:00-18:00）

QQ ：1570468124

手机：18915418616

官网：http://www.medchemexpress.com/

快速导航：

公司介绍

产品中心

新闻动态

在线咨询

联系我们

公司介绍

产品中心

新闻动态

在线咨询

联系我们

总部地址：

江苏省苏州市工业园区星湖街218号 苏州生物医药产业园一期（生物纳米园）A4-216(邮编：215125)

工作时间：周一至周五9:00~18:00

技术支持：

Email：info@ebiomall.com

短信：18915418616

服务热线：

4000-520-616（全国）

☏  0512-67156496（苏州）

版权信息：

©  2015-2022 苏州蚂蚁淘生物科技有限公司 版权所有 中国

网站备案：

苏ICP备17049038号-1

苏公网安备 32059002001627号

友情链接：

联系QQ:764052152

medix代购 medkoo正品 megazyme清关 microspheres官网 midlandsci报价 minerva采购 molecular molinnov moltox mpbio relassay产品 ​​polysciences药物筛选 Encapsula公司 viskase 28mm MD44 Apin产品代理 美国Molecular Research Immunology Consultan 蚂蚁淘 广东广洁净化设备有限公司

免责声明：

本站有部分内容来自互联网，如无意中侵犯了某个媒体 、公司 、企业或个人等的知识产权，请来电或致函告之，
本网站将在规定时间内给予删除等相关处理。

扫描二维码关注官方微信

获取最新促销及产品信息