RS-25344-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERS-25344hydrochlorideCat.No.:HY-108621CASNo.:152815-28-6分?式:C??H??ClN?O?分?量:411.8作?靶點:Phosphodiesterase(PDE)作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:83.33mg/mL(202.36mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.4284mL12.1418mL24.2836mL5mM0.4857mL2.4284mL4.8567mL10mM0.2428mL1.2142mL2.4284mL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。-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(dāng)?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(dāng)保存；體內(nèi)實驗的?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:≥2.08mg/mL(5.05mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.05mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.05mM);ClearsolutionBIOLOGICALACTIVITY?物活性RS-25344hydrochloride?種選擇性cAMP-磷酸?酯酶4(PDEIV)抑制劑，在?淋巴細胞中的IC50為0.28nM，對PDEI、II、III僅具有微弱的抑制作?，IC50分別為>100μM、160μM、330μM。RS-25344hydrochloride具有抗炎、增強記憶?和認知能?以及抗腫瘤作?。IC50&TargetPDEⅣPDEⅠPDEⅡPDEⅢ0.28nM(IC50)>100μM(IC50)160μM(IC50)330μM(IC50)體外研究RS-25344hydrochloride(0-10μM)isapotentinhibitorofspermPDEactivity,withaneffectiveconcentrationof0.3nMandreachingmaximuminhibitionintherangeof100nM[2].體內(nèi)研究RS-25344hydrochloride(5mg/kg;i.p.;twicedailyfor72h)resultsinsignificantincreasesinstomachweightsinwildtypeC57BL/6mice[3].RS-25344hydrochloride(1mg/kg;i.p.;30minpriortofoodbolus)increasesgastricretentioninmice[3].REFERENCES[1].WillMcDonough,etal.PAN-selectiveinhibitionofcAMP-phosphodiesterase4(PDE4)inducesgastroparesisinmice.FASEBJ.2020Sep;34(9):12533-12548.[2].JDFisch,etal.Enhancementofmotilityandacrosomereactioninhumanspermatozoa:differentialactivationbytype-specificphosphodiesteraseinhibitors.HumReprod.1998May;13(5):1248-54.[3].TKaneko,etal.ElevatedintracellularcyclicAMPinhibitschemotaxisinhumaneosinophils.CellSignal.1995Jul;7(5):527-34.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forre