Dacarbazine-citrate-Imidazole-Carboxamide-citrate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEDacarbazinecitrateCat.No.:HY-B0078ACASNo.:64038-56-8Synonyms:ImidazoleCarboxamidecitrate分⼦式:C₁₂H₁₈N₆O₈分⼦量:374.31作⽤靶点:Apoptosis作⽤通路:Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Dacarbazinecitrate⼀种细胞周期⾮特异性抗肿瘤烷化剂。Dacarbazinecitrate抑制T和B淋巴细胞反应，IC50分别为50和10μg/mL。Dacarbazinecitrate可⽤于凋亡和多种癌症如转移性恶性⿊⾊素瘤的研究。体外研究DacarbazinecitratehaslesspronouncedinhibitionofmitogenesiswithIC50valuesof50and10μg/mLforTandBcells,respectively[2].Dacarbazinecitrate(30μM,0-14min)evokesaconcentration-dependentcalciumresponseinhTRPA1-HEK293cellswithanEC50valueof23μMandselectivelyactivatesthehumanTRPA1channel[3].Dacarbazinecitrate(100-10,000μM,24h)hascytotoxicactiononB16-F10melanomacells[3].CellViabilityAssay[3]CellLine:B16-F10cellConcentration:100-10,000μMIncubationTime:24hResult:Reducedcellviabilityto3,000and10,000uM,withaninhibitionpercentageof62±2%after24hofincubation.体内研究Dacarbazinecitrate(1mg/kg,i.p.)evokesaconcentration-dependentcalciumresponseandthemaximumcalciumresponsewithanEC50valueof16μMinasubsetofcellsofculturedmouseDRGneuronsandexcitesTRPA1inrodentsensoryneurons[3].1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEDacarbazinecitrate(1mg/kg,i.p.;1,3,5and7daysforchronicpainor1mg/kg,i.p.foracutetreatment)inducesmechanicalandcoldallodyniainmice[3].Dacarbazinecitrate-inducednociceptioncanbereducedbyTRPA1-deficientmiceandantisenseoligonucleotidefortheTRPA1receptor[3].Dacarbazinecitrate-inducedchronicnociceptioncanbereducedbyselectiveTRPA1receptorantagonistsandantioxidants[3].Dacarbazinecitrate-inducednociceptioncanberesistedbyRPA1antagonistoranantioxidantinatumor-associatedcancerpainmodel[3].AnimalModel:C57BL/6,Trpa1+/+orTrpa1−/−mice[3]Dosage:1mg/kgAdministration:1mg/kg,i.p.(foracutetreatment);1mg/kg,i.p.;1,3,5and7days(forchronicpain)Result:Causedmechanicalallodyniawithacuteorrepeatedadministration.户使⽤本产品发表的科研⽂献•Theranostics.2020Jul25;10(21):9477-9494.•JMolMed(Berl).2019Aug;97(8):1183-1193.•ExpCellRes.2020Aug1;393(1):112054.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].AbdullahAAl-Badr,etal.Dacarbazine.ProfilesDrugSubstExcipRelatMethodol[2].JMRojo,etal.InhibitionofTandBlymphoblasticresponsebymithramycin,dacarbazine,prospidiumchlorideandpeptichemio.Chemotherapy.1983;29(5):345-51.[3].IntJCancer,etal.Dacarbazinealoneorassociatedwithmelanoma-bearingcancerpainmodelinducespainfulhypersensitivitybyTRPA1activationinmice.IntJCancer.2020May15;146(10):2797-2809.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformed