SB-452533-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESB452533Cat.No.:HY-108458CASNo.:459429-39-1分?式:C??H??BrN?O分?量:376.29作?靶點:TRPChannel作?通路:MembraneTransporter/IonChannel;NeuronalSignaling儲存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(265.75mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.6575mL13.2876mL26.5752mL5mM0.5315mL2.6575mL5.3150mL10mM0.2658mL1.3288mL2.6575mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.64mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(6.64mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.64mM);ClearsolutionBIOLOGICALACTIVITY?物活性SB452533?種有效的選擇性TRPV1拮抗劑，pKb為7.8[1]。體外研究SB452533ispotentasanantagonistattheclonedrecombinantratTRPV1receptorinHEK293cellswithapKbof7.7andapIC50of7.0[1].SB-452533reducesphosphorylationofCAMKK2andAMPK[2].WesternBlotAnalysis[2]CellLine:Skeletalmuscle(C2C12)cellsConcentration:0,50,100,200,and400μMIncubationTime:30minutes;followedby200μMCapsaicintreatmentforanother30min.Result:SignificantlyreducedCapsaicin-inducedphosphorylationofAMPKandCAMKK2.體內(nèi)研究Capsaicin(Cap;smalldose2mg/kg)significantlyreducesBleomycin-inducedpulmonaryfibrosisinmice.SB-452533abolishestheeffectsofsmalldoseCap[3].AnimalModel:BALB/cmicebearingpulmonaryfibrosismodel[3]Dosage:2.5mg/kgAdministration:Treatmentreceiveddailydrugviasubcutaneousinjectionfor21daysResult:Theeffect(reducedBleomycin-inducedpulmonaryfibrosis)ofCapwereabolishedinthepresenceofSB-452533.REFERENCES[1].HarshadKRami,etal.DiscoveryofsmallmoleculeantagonistsofTRPV1.BioorgMedChemLett.2004Jul16;14(14):3631-4.[2].ParisaVahidiFerdowsi,etal.TRPV1ActivationbyCapsaicinMediatesGlucoseOxidationandATPProductionIndependentofInsulinSignallinginMouseSkeletalMuscleCells.Cells.2021Jun21;10(6):1560.[3].LinMingLu,etal.Effectofsmalldosecapsaicinfortreatmentofpulmonaryfibrosisinmiceanditsmechanism.ZhongguoYingYongShengLiXueZaZhi.2020May;36(3):216-222.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap