Exendin-4,a39aminoacidpeptide,isalong-actingglucagon-likepeptide-1receptoragonistwithanIC₅₀of3.22nM.

IC50:3.22nM(glucagon-likepeptide-1receptor)^[1]

Inhumanumbilicalveinendothelialcells,exendin-4significantlyincreasesNOproduction,endothelialNOsynthase(eNOS)phosphorylation,andGTPcyclohydrolase1(GTPCH1)levelinadose-dependentmanner^[2].Exendin-4showscytotoxiceffectstoMCF-7breastcancercellswithIC₅₀of5μMat48hour^[3].

Bothlow-andhigh-doseexendin-4treatmentinob/obmiceimproveserumALTandreduceserumglucose,insulinlevelsandcalculatedHOMAscorescomparedwithcontrol.Exendin-4-treatedob/obmicesustainamarkedreductioninthenetweightgaininthefinal4weeksofthestudyperiod^[4].Animalstreatedwithexendin-4havemorepancreaticacinarinflammation,morepyknoticnucleiandweighsignificantlylessthancontrolrats.Exendin-4treatmentisassociatedwithlowerinsulinandleptinlevelsaswellaslowerHOMAvaluesinrats^[5].Exenatidecausesdose-dependentrelaxationofratthoracicaorta,whichisevokedviatheGLP-1receptorandismediatedmainlybyH₂SbutalsobyNOandCO^[6].

• [1].DoyleME,etal.Theimportanceofthenine-aminoacidC-terminalsequenceofexendin-4forbindingtotheGLP-1receptorandforBIOLOGicalactivity.RegulPept.2003Jul15;114(2-3):153-8.

  [2].WeiR,etal.ExenatideexertsdirectprotectiveeffectsonendothelialcellsthroughtheAMPK/Akt/eNOSpathwayinaGLP-1receptor-dependentmanner.AmJPhysiolEndocrinolMetab.2016Jun1;310(11):E947-57.

  [3].Fidan-YaylalıG,etal.Antidiabeticexendin-4activatesapoptoticpathwayandinhibitsgrowthofbreastcancercells.TumourBiol.2016Feb;37(2):2647-53.

  [4].DingX,etal.Exendin-4,aglucagon-likeprotein-1(GLP-1)receptoragonist,reverseshepaticsteatosisinob/obmice.Hepatology.2006Jan;43(1):173-81.

  [5].NachnaniJS,etal.Biochemicalandhistologicaleffectsofexendin-4(exenatide)ontheratpancreas.Diabetologia.2010Jan;53(1):153-9.

  [6].SélleyE,etal.Exenatideinducesaorticvasodilationincreasinghydrogensulp,carbonmonoxideandnitricoxideproduction.CardiovascDiabetol.2014Apr2;13:69.

Rat:20Sprague-Dawleymalerats,tenofwhicharetreatedwithexendin-4(10μg/kg)andtenofwhichareusedascontrols.Thestudyperiodis75days.Serumandpancreatictissueareremovedforbiochemicalandhistologicalstudy.Bloodglucose,amylase,lipase,insulinandADIpocytokinesarecomparedbetweenthetwogroups^[5].

Mouse:Theexendin-4treatmentgroupsaretreatedwith10μg/kgevery24hoursforthefirst14days.Thistreatmentistheinductionphase.Respectivecontrolmice(leanandob/ob)receivesalineevery24hours.After14daysExendin-4-treatedmicearerandomlydividedintotwogroups:onegroupreceiveshighdoseexendin-4(20μg/kg)every12hours,whilethesecondgroupcontinueswithlowdoseexendin-4(10μg/kg)every12hours.Thecontrolmicecontinuetoreceivesalineevery12hours.Themiceareweigheddailyforthe60-daytreatmentperiod^[4].

• [1].DoyleME,etal.Theimportanceofthenine-aminoacidC-terminalsequenceofexendin-4forbindingtotheGLP-1receptorandforbiologicalactivity.RegulPept.2003Jul15;114(2-3):153-8.

  [2].WeiR,etal.ExenatideexertsdirectprotectiveeffectsonendothelialcellsthroughtheAMPK/Akt/eNOSpathwayinaGLP-1receptor-dependentmanner.AmJPhysiolEndocrinolMetab.2016Jun1;310(11):E947-57.

  [3].Fidan-YaylalıG,etal.Antidiabeticexendin-4activatesapoptoticpathwayandinhibitsgrowthofbreastcancercells.TumourBiol.2016Feb;37(2):2647-53.

  [4].DingX,etal.Exendin-4,aglucagon-likeprotein-1(GLP-1)receptoragonist,reverseshepaticsteatosisinob/obmice.Hepatology.2006Jan;43(1):173-81.

  [5].NachnaniJS,etal.Biochemicalandhistologicaleffectsofexendin-4(exenatide)ontheratpancreas.Diabetologia.2010Jan;53(1):153-9.

  [6].SélleyE,etal.Exenatideinducesaorticvasodilationincreasinghydrogensulp,carbonmonoxideandnitricoxideproduction.CardiovascDiabetol.2014Apr2;13:69.

4186.57

C₁₈₄H₂₈₂N₅₀O₆₀S

141758-74-9

RoomtemperatureincontinentalUS;mayvaryelsewhere

DMSO:≥32mg/mL;H₂O:1.23mg/mL(Needultrasonicandwarming)

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

Purity:98.96%

SelectBatch:HY-13443-21056HY-13443-25694

DataSheet(132KB)SDS(120KB)

COA(94KB)RP-HPLC(242KB)MS(226KB)

HandlingInstructions(1252KB)

• [1].DoyleME,etal.Theimportanceofthenine-aminoacidC-terminalsequenceofexendin-4forbindingtotheGLP-1receptorandforbiologicalactivity.RegulPept.2003Jul15;114(2-3):153-8.

  [2].WeiR,etal.ExenatideexertsdirectprotectiveeffectsonendothelialcellsthroughtheAMPK/Akt/eNOSpathwayinaGLP-1receptor-dependentmanner.AmJPhysiolEndocrinolMetab.2016Jun1;310(11):E947-57.

  [3].Fidan-YaylalıG,etal.Antidiabeticexendin-4activatesapoptoticpathwayandinhibitsgrowthofbreastcancercells.TumourBiol.2016Feb;37(2):2647-53.

  [4].DingX,etal.Exendin-4,aglucagon-likeprotein-1(GLP-1)receptoragonist,reverseshepaticsteatosisinob/obmice.Hepatology.2006Jan;43(1):173-81.

  [5].NachnaniJS,etal.Biochemicalandhistologicaleffectsofexendin-4(exenatide)ontheratpancreas.Diabetologia.2010Jan;53(1):153-9.

  [6].SélleyE,etal.Exenatideinducesaorticvasodilationincreasinghydrogensulp,carbonmonoxideandnitricoxideproduction.CardiovascDiabetol.2014Apr2;13:69.

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官网 medkoo采购 megazyme报价 microspheres代购 midlandsci正品 minerva清关 molecular molinnov moltox mpbio Virusys中国 polysciences磁珠 安玛西亚公司 BSGLDN试剂盒 coynechemical产品代理 Xcess DB Biotech代理 蚂蚁淘 生化酶类

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