AMTB-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAMTBhydrochlorideCat.No.:HY-100345CASNo.:926023-82-7分?式:C??H??ClN?O?S分?量:430.99作?靶點(diǎn):TRPChannel作?通路:MembraneTransporter/IonChannel;NeuronalSignaling儲(chǔ)存?式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(232.02mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.3202mL11.6012mL23.2024mL5mM0.4640mL2.3202mL4.6405mL10mM0.2320mL1.1601mL2.3202mL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(sealedstorage,awayfrommoistureandlight)。-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:≥2.5mg/mL(5.80mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(5.80mM);Clearsolution;Needultrasonic1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.80mM);ClearsolutionBIOLOGICALACTIVITY?物活性AMTBhydrochloride?種選擇性TRPM8通道阻滯劑。AMTBhydrochloride抑制icilin誘導(dǎo)的TRPM8通道激活，pIC50為6.23。AMTBhydrochloride可?于膀胱過(guò)度活動(dòng)和膀胱疼痛綜合征的研究。AMTBhydrochloride電壓門(mén)控鈉通道的?選擇性抑制劑(NaV)。體外研究AMTBhydrochlorideblocksveratridine-inducedmembranepotentialchangesateachNaV1isoform(pIC50sranging4.83-5.69forNaV1.1-NaV1.8)[2].AMTBhydrochloridedecreasesviablecellnumberinMDA-MB-231andSK-BR-3breastcancercelllines(30and100μM),andalsoreducesthemigrationofMDA-MB-231cells(30μM)[2].體內(nèi)研究Intheanesthetizedrat,AMTB(3mg/kg;intravenous)hydrochloridedecreasesthefrequencyofvolume-inducedbladdercontractions,withoutreducingtheamplitudeofcontraction[1].REFERENCES[1].LashingerES,etal.AMTB,aTRPM8channelblocker:evidenceinratsforactivityinoveractivebladderandpainfulbladdersyndrome.AmJPhysiolRenalPhysiol.2008;295(3):F803-F810.[2].YapaKTDS,etal.AssessmentoftheTRPM8inhibitorAMTBinbreastcancercellsanditsidentificationasaninhibitorofvoltagegatedsodiumchannels.LifeSci.2018;198:128-135.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forre