RN-1734-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERN-1734Cat.No.:HY-19975CASNo.:946387-07-1分?式:C??H??Cl?N?O?S分?量:353.31作?靶點(diǎn):TRPChannel作?通路:MembraneTransporter/IonChannel;NeuronalSignaling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:25mg/mL(70.76mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.8304mL14.1519mL28.3038mL5mM0.5661mL2.8304mL5.6608mL10mM0.2830mL1.4152mL2.8304mL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(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥3.25mg/mL(9.20mM);Clearsolution1/3MasterofBioactiveMolecules—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:≥3.25mg/mL(9.20mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥3.25mg/mL(9.20mM);ClearsolutionBIOLOGICALACTIVITY?物活性RN-1734?種選擇性TRPV4通道拮抗劑，完全拮抗4αPDD介導(dǎo)的TRPV4活化，作?于hTRPV4,mTRPV4,和rTRPV4，IC50分別為2.3μM、5.9μM、3.2μM[1]。RN-1734能明顯降低腫瘤壞死因?α(TNF-α)和?細(xì)胞介素1β(IL-1β)的產(chǎn)?，?不改變olig2-陽(yáng)性細(xì)胞的數(shù)量[2]。IC50&TargetIC50:2.3μM(hTRPV4),5.9μM(mTRPV4),3.2μM(rTRPV4)[1]體外研究RN-1734(27hours;10μM)reversestheincreaseintheapoptoticrateofoligodendrocytesinducedbyCM(LPS-activatedmicrogliagroup)apoptosis[2].RN-1734(27hours;10μM)alleviatesCM-induceddecreasesinCNP[2].ApoptosisAnalysis[2]CellLine:MicroglialcellsConcentration:27hoursIncubationTime:10μMResult:Significantlydecreasedthepercentageofcleaved-caspase3positivecells.WesternBlotAnalysis[2]CellLine:MicroglialcellsConcentration:27hoursIncubationTime:10μMResult:AlleviatedCM(withLPSonly)-induceddecreasesinCNP.體內(nèi)研究RN-1734(0.5μl;microinjectorpump;dailyfor5weeks)significantlyreversesthedecreaseinCNPproteinandimprovesmyelinationinCPZ-induceddemyelinationmouse[2].AnimalModel:CPZ-induceddemyelinationmousemodel(C57BL/6malemice)[2]Dosage:0.5μl(10μMin5%DMSOand0.9%NaCl)Administration:Microinjectorpumpfor5weeks2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEResult:SignificantlyreversedthedecreaseinCNPproteinandimprovedmyelinationinCPZ-induceddemyelinationmouse.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?JBiolChem.2022May;298(5):101847.?AcsBiomaterSciEng.2019Dec9;5(12):6520-6529.?PLoSOne.2019Jun10;14(6):e0217511.?BiolBull.2022Feb.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].KatoK,etal.Acidosisenvironmentpromotesosteoclastformationbyactingonthelastphaseofpreosteoclastdifferentiation:astudytoelucidatetheactionpointsofacidosisandsearchforputativetargetmolecules.EurJPharmacol.2011Aug1;663(1-[2].VincentF,etal.IdentificationandcharacterizationofnovelTRPV4modulators.BiochemBiophysResCommun.2009Nov20;389(3):490-4.[3].LiuM,etal.TRPV4InhibitionImprovedMyelinationandReducedGliaReactivityandInflammationinaCuprizone-InducedMouseModelofDemyelination.FrontCellNeurosci.2018Nov5;12:392.McePdfHeightCaution:Producthasnotbee