WS-12-AR-15512-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEWS-12Cat.No.:HY-108449CASNo.:68489-09-8Synonyms:AR-15512;AVX-012分?式:C??H??NO?分?量:289.41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:20mg/mL(69.11mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.4553mL17.2765mL34.5531mL5mM0.6911mL3.4553mL6.9106mL10mM0.3455mL1.7277mL3.4553mL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>>90%cornoil1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2mg/mL(6.91mM);ClearsolutionBIOLOGICALACTIVITY?物活性WS-12(AR-15512)?種強(qiáng)效和選擇性的TRPM8激動(dòng)劑，薄荷醇的衍?物，作為?種冷卻劑。WS-12顯?出鎮(zhèn)痛作?，可?于慢性神經(jīng)性疼痛的研究。IC50&TargetEC50:39nM(TRPM8)[1]體外研究WS-12(10μM)showsTRPM8agonismintestsonheterologouslyexpressedTRPionchannels[1].WS-12(1or10μM;0-250s)showshighlypotentandspecificTRPM8channelagonistinDRGneurons[1].CellViabilityAssay[1]CellLine:HEK293TcellsConcentration:10μMIncubationTime:Result:ActivatedmouseTRPM8(mTRPM8),butneitheractivatednorinhibitedmTRPA1.CellViabilityAssay[1]CellLine:CulturedmouseDRGneuronsConcentration:1or10μMIncubationTime:0-250sResult:Showedapproximately10%to14%ofculturedwild-typeneuronsresponsivetoWS-12.體內(nèi)研究WS-12(intraperitonealinjection;10mg/kg;once)showsanalgesiceffectbyselectiveTRPM8activationinmice[1].AnimalModel:Trpm8–/–miceandmiceinjectedwithCapsaicin[1]Dosage:10mg/kgAdministration:Intraperitonealinjection;10mg/kg;onceResult:Producedanobviousanalgesiceffect,andthiseffectabolishedinTrpm8–/–mice.Showednochangefallinglatenciesinmiceintherotarodtest.ReducedCapsaicin-inducednocifensivebehavior.REFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].MaS,etal.MentholderivativeWS-12selectivelyactivatestransientreceptorpotentialmelastatin-8(TRPM8)ionchannels.PakJPharmSci.2008Oct;21(4):370-8.[2].BeckB,etal.Prospectsforprostatecancerimagingandtherapyusinghigh-affinityTRPM8activators.CellCalcium.2007Mar;41(3):285-94.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.F