Rimcazole-dihydrochloride-BW-234U-dihydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERimcazoledihydrochlorideCat.No.:HY-108510CASNo.:75859-03-9Synonyms:BW234Udihydrochloride分?式:C??H??Cl?N?分?量:394.38作?靶點:SigmaReceptor;DopamineReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲存?式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性數(shù)據(jù)體外實驗DMSO:12.5mg/mL(31.70mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.5356mL12.6781mL25.3563mL5mM0.5071mL2.5356mL5.0713mL10mM0.2536mL1.2678mL2.5356mL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(sealedstorage,awayfrommoistureandlight)。-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:≥1.25mg/mL(3.17mM);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:≥1.25mg/mL(3.17mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥1.25mg/mL(3.17mM);ClearsolutionBIOLOGICALACTIVITY?物活性Rimcazole(BW234U)dihydrochloride?種咔唑衍?物，部分?作σ受體拮抗劑。Rimcazoledihydrochloride以中等親和?結(jié)合多巴胺轉(zhuǎn)運蛋?并抑制多巴胺攝取。Rimcazoledihydrochloride可以減弱可卡因誘導(dǎo)的運動活動和致敏作?。Rimcazoledihydrochloride也可?于癌癥的研究。IC50&Targetsigma(σ)receptor[1]dopaminetransporter[1]體外研究Rimcazole(1-50μM;24-48h)concentration-dependentlydecreasesthenumberHCT-116p53+/+cells[2].Rimcazole(50μM;1-24h)dihydrochlorideinducesatransientaccumulationofHIF-1αproteiincancercells(HCT-116p53+/+andMDAMB231cells)butnotinnormalhumandermalfibroblasts[2].WesternBlotAnalysis[2]CellLine:HCT-116p53+/+cellsConcentration:50μMIncubationTime:1,2,3,5,6,24hoursResult:AccumulationofHIF-1αprotein,maximalat6?h.Nochangeinp53proteinlevels.HIF-1αproteinlevelsreturnedtonormalsteady-statelevelswithin24?h.REFERENCES[1].GilmoreDL,et,al.Reviewofthepharmacologicalandclinicalprofileofrimcazole.CNSDrugRev.Spring2004;10(1):1-22.[2].AchisonM,et,al.HIF-1alphacontributestotumour-selectivekillingbythesigmareceptorantagonistrimcazole.Oncogene.2007Feb22;26(8):1137-46.[3].MatsumotoRR,et,al.Rimcazoleanalogsattenuatetheconvulsiveeffectsofcocaine:correlationwithbindingtosigmareceptorsratherthandopaminetransporters.Neuropharmacology.2001Dec;41(7):878-86.[4].JobMO,et,al.Abehavioraleconomicanalysisoftheeffectsofrimcazoleonreinforcingeffectsofcocaineinjectionandfoodpresentationinrats.Psychopharmacology(Berl).2019Dec;236(12):3601-3612.McePdfHeightCaution:Producthasnotbeenfullyvalidatedform