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Medchemexpress/Z-VAD-FMK(Synonyms: Z-VAD(OMe)-FMK; Z-Val-Ala-Asp(OMe)-FMK)/HY-16658/5mg
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Description | Z-VAD-FMKisacell-permeable,pan-caspaseinhibitor. |
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IC50&Target | pan-caspase[1] |
InVitro | Z-VAD-FMKisabroad-spectrumcaspaseinhibitor,hasbeenshowntoinhibittheintracellularactivationofcaspase-likeproteases.TheinjectionofZ-VAD-FMKsuppressesthecaspase-3activityinlungtissues,andsignificantlydecreasesthenumberofterminaldUTPnick-endlabeling-positivecells[1].Z-VAD-FMKisadmiNISTeredintraperitoneallyat1hourbeforeand6hoursafterSAH.Expressionofcaspase-3andpositiveTUNELisexaminedasMarkersforapoptosis.Z-VAD-FMKsuppressesTUNELandcaspase-3staininginendothelialcells,decreasescaspase-3activation,reducesBBBpermeABIlity,relievesvasospasm,abolishesbrainedema,andimprovesneurologicaloutcome[2].Z-VAD-FMKisacell-permeablecaspaseinhibitor,efficientlyblockscelldeathinducedbySMNdeficiency[3]. |
InVivo | ThesurvivalrateofmiceisprolongedsignificantlybytheinjectionofZ-VAD-FMK.AllmicesuccumbedtoLPSwithin30hours.Bycontrast,themicetreatedwithZ-VAD-FMKsurvivesignificantlylongerand27%ofthemicesurvivedmorethan7days[1]. |
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CellAssay [3] | Z-VAD-FMKisdissolvedinDMSOandstored,andthendilutedwithappropriatemediumbeforeuse[3]. PCRproductscontainingcodingsequencesforthedSMN(forwardprimer:5′-TAATACGACTCACTATAGGGAAGACGTACGACGAGTCG-3′;andreverseprimer:5′-TAATACGACTCACTATAGGGGTGGTGCTGGCTTCTTTC-3′;productlength,601bps;boldanditalicslettersrepresentT7promotersequences)andcontrolDrosophilaPresenilin(dPsn)gene(forwardprimer:5′-TAATACGACTCACTATAGGGTGGCTGCTGTCAATCTC-3′;andreverseprimer:5′-TAATACGACTCACTATAGGGCGATAGCAACGCTTCTTG-3′;productlength:543bps)areobtainedandgel-purified.Double-strandedRNAs(dsRNA)aregeneratedbytranscriptionwithRibomaxT7TranscriptionkitanddigestedwithRnase-freeDNase.ThedsRNAproductsareethanolprecipitatedandannealedbyincubationat65°Cfor30minandthenslowlyallowedtocoolatroomtemperature.TheannealeddsRNAproductsareanalyzedona1%agaorsegeltoensurethemajorityofdsRNAexistedasasingleband.ThedsRNA(2μg)and/orplasmidDNAs(2μg)areintroducedintocellsbyusingCellfectin.Caspaseinhibitionisachievedbyusing50μMofZ-VAD-FMKintheculturemedium[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly. | ||||||||||||||||
AnimalAdministration [1][2] | Z-VAD-FMKisdissolvedat2mg/mLin1%DMSOinsterilesaline(Mice)[1]. Mice[1] | ||||||||||||||||
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MolecularWeight | 467.49 | ||||||||||||
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Formula | C₂₂H₃₀FN₃O₇ | ||||||||||||
CASNo. | 187389-52-2 | ||||||||||||
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Shipping | RoomtemperatureincontinentalUS;mayvaryelsewhere | ||||||||||||
Solvent&Solubility | DMSO:≥30mg/mL *"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">1> Purity:>98.0% 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
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