RHC-80267-U-57908-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERHC80267Cat.No.:HY-107416CASNo.:83654-05-1Synonyms:U-57908分?式:C??H??N?O?分?量:394.51作?靶點(diǎn):Acyltransferase;mAChR;COX;Phospholipase作?通路:MetabolicEnzyme/Protease;GPCR/GProtein;NeuronalSignaling;Immunology/Inflammation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(63.37mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.5348mL12.6740mL25.3479mL5mM0.5070mL2.5348mL5.0696mL10mM0.2535mL1.2674mL2.5348mL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)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.34mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.34mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.34mM);ClearsolutionBIOLOGICALACTIVITY?物活性RHC80267(U-57908)?種有效的選擇性?酰?油脂酶(DAGL)抑制劑(對(duì)???板的IC50為4μM)。RHC80267抑制膽堿酯酶活性，IC50為4μM，從?增強(qiáng)了?酰膽堿引起的松弛。RHC80267還抑制COX活性和磷脂酰膽堿的?解。IC50&TargetIC50:4μM(Caninediacylglycerollipase),4μM(Cholinesterase);COX;Phosphatidylcholine[1][3][4]體外研究ThepotentiationbyRHC80267oftherelaxationtoacetylcholinecouldbecausedbytheinhibitionofcholinesterase:(1)RHC80267doesnotaffecttheresponsestocarbachol,thecarbamylderivativeofacetylcholinewhichonlydiffersfromacetylcholinebyitsresistancetohydrolysisbycholinesterase,and(2)theeffectofRHC80267ismimickedbytheinhibitorofcholinesteraseneostigmine,RHC80267showingnoadditionaleffectinthepresenceofamaximallyeffectiveconcentrationofneostigmine.ThedeterminationoftheeffectofRHC80267onthecholinesteraseactivityofbrainhomogenateconfirmedthatRHC80267inhibitsthisenzymeinthesamerangeofconcentrationsincreasingtherelaxationtoacetylcholine,namelyat1-10μM[2].體內(nèi)研究RHC80267(40μM)enhancescontractionsinducedbyU46619(athromboxaneA2analog)inhumanandratpulmonaryarteries(hPAsandrPAs,respectively)andbyangiotensinII(ANGII)inrPAsinanendothelium-dependentmanner[3].REFERENCES[1].SutherlandCA,etal.RelativeactivitiesofratanddogplateletphospholipaseA2anddiglyceridelipase.SelectiveinhibitionofdiglyceridelipasebyRHC80267.JBiolChem.1982Dec10;257(23):14006-10.[2].GhisdalP,etal.ThediacylglycerollipaseinhibitorRHC-80267potentiatestherelaxationtoacetylcholineinratmesentericarterybyanti-cholinesteraseaction.EurJPharmacol.2005Jul4;517(1-2):97-102.[3].KarpińskaO,etal.ActivationofCB1receptorsby2-arachidonoylglycerolattenuatesvasoconstrictioninducedbyU46619andangiotensinIIinhumanandratpulmonaryarteries.AmJPhysiolRegulIntegrCompPhysiol.2017Jun1;312(6):R883-R893.[4].OglesbyTD,etal.TheinhibitionofarachidonicacidmetabolisminhumanplateletsbyRHC80267,adiacylglycerollipaseinhibitor.BiochimBiophysActa.1984Apr18;793(2):269-77.McePdfHeightCaution:Producthasnotbee