Protirelin-acetate-Thyrotropin-releasing-hormone-acetate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEProtirelinacetateCat.No.:HY-P0002ACASNo.:120876-23-5Synonyms:Thyrotropin-releasing-hormoneacetate;TRHacetate分⼦式:C₁₆H₂₂N₆O₄.₃/₂C₂H₄O₂分⼦量:452.46Sequence:{pGlu}-His-Pro-NH2SequenceShortening:{pGlu}-HP-NH2作⽤靶点:ThyroidHormoneReceptor作⽤通路:Others储存⽅式:Sealedstorage,awayfrommoisturePowder-80°C2years-20°C1yearInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(552.54mM;Needultrasonic)H2O:50mg/mL(110.51mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2101mL11.0507mL22.1014mL5mM0.4420mL2.2101mL4.4203mL10mM0.2210mL1.1051mL2.2101mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.60mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.60mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.60mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性ProtirelinAcetate⼀种⾼度保守的神经肽，发挥促甲状腺激素(TSH)⽔平的激素控制作⽤，及神经调节功能。IC50&TargetThyroidhormonereceptor体内研究Protirelin(TRH)isanevolutionarilyancientneuropeptide,havingitsoriginbeforethedivergenceofprotostomesanddeuterostomes,andmayancestrallyhavebeeninvolvedinthecontrolofpostembryonicgrowthandreproduction[1].Theeffectofthethyrotropin-releasinghormone(Protirelin,TRH),oneofthehypothalamicreleasinghormones,onbodytemperatureisinvestigatedintherat.Protirelin,indosesof1,5,10and20mg/kg,isinjectedintraperitoneallytomaleWistarratsweighing200-250g.Protirelincausesatemporaryriseinbodytemperaturedose-dependently.Thethyroidectomizedratsinjected20mg/kgofProtirelinwhichinducesasignificanthyperthermiainthesham-operatedanimals,failtoshowariseinbodytemperature.ThepresentresultssuggestthatareleaseofthyroidhormonemightparticipateinthehyperthermicactionofProtirelin[2].PROTOCOLAnimalRats[2]Administration[2]NinetymaleWistarratsweighing200-250garesubjectedtothestudy.Inthefirstexperiment,50ratsaredividedintofivegroupsrandomly.FourdosesofProtirelindissolvedinphysiologicalsaline,i.e.,1mg/kg,5mg/kg,10mg/kgand20mg/kg,areadministeredintraperitoneallytothefourgroupsandsalinetotheremainingcontrolgroup.Rectaltemperatureismeasuredattheplace5cminnerfromtheanuswiththeelectronicthermisterbeforeandaftertreatmentwithProtirelinorsaline.Inthesecondexperiment,40ratsarethyroidectomizedorsham-operatedundertheanesthesiabythiopentalsodium.Tendaysaftertheoperation,20mg/kgofProtirelinorsalineisadministeredtothethyroidectomizedandsham-operatedanimalsbyi.p.andrectaltemperatureismeasuredusingthesamemethodasusedinthefirstexperiment.Thesetwoexperimentsareundertakenfrom1p,m,to4p.m.andtheroomtemperatureiskeptat24±1°Cthroughtheexperimentsincludingthebreedingperiod.Forastatisticalanalysis,Student'sttest(two-tailed)isadopted.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].VanSinayE,etal.EvolutionarilyconservedTRHneuropeptidepathwayregulatesgrowthinCaenorhabditiselegans.ProcNatlAcadSciUSA.2017May16;114(20):E4065-E4074.[2].NodaY,etal.Hyperthermiainducedbythyrotropin-releasinghormone(TRH,Protirelin)intherat.KurumeMedJ.1979;26(2):107-12.McePdfHeigh