AT2-receptor-agonist-C21-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAT2receptoragonistC21Cat.No.:HY-100113CASNo.:477775-14-7分?式:C??H??N?O?S?分?量:475.62作?靶點(diǎn):AngiotensinReceptor作?通路:GPCR/GProtein儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(210.25mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.1025mL10.5126mL21.0252mL5mM0.4205mL2.1025mL4.2050mL10mM0.2103mL1.0513mL2.1025mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.37mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.37mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.37mM);ClearsolutionBIOLOGICALACTIVITY?物活性AT2receptoragonistC21?種類(lèi)似藥物的，選擇性angiotensinIIAT2receptor(?管緊張素IIAT2受體)激動(dòng)劑，對(duì)AT2受體和AT1受體的Ki值分別為0.4nM和10μM。IC50&TargetKi:0.4nM(AT2)and>10μM(AT1)[1]體內(nèi)研究AT2receptoragonistC21,withabioavailabilityof20-30%afteroraladministrationandahalf-lifeestimatedto4hinrat,inducesoutgrowthofneuritecells,stimulatesp42/p44mapk,enhancesinvivoduodenalalkalinesecretioninSprague-Dawleyrats,andlowersthemeanarterialbloodpressureinanesthetized,spontaneouslyhypertensiverats[1].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?ClinSci.2022Jun13;CS20220236.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].WanY,etal.Design,synthesis,andbiologicalevaluationofthefirstselectivenonpeptideAT2receptoragonist.JMedChem.2004Nov18;47(24):5995-6008.[2].SchwengelK,NamsolleckP,LuchtK,etal.AngiotensinAT2-receptorstimulationimprovessurvivalandneurologicaloutcomeafterexperimentalstrokeinmice.JMolMed(Berl).2016;94(8):957-966.[3].FatimaN,PatelS,HussainT.AngiotensinAT2ReceptorisAnti-inflammatoryandReno-ProtectiveinLipopolysaccharideMiceModel:RoleofIL-10.FrontPharmacol.2021;12:600163.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forres