Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEKB-5492anhydrousCat.No.:HY-19120CASNo.:129200-10-8分?式:C??H??N?O??分?量:546.57作?靶點:SigmaReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:250mg/mL(457.40mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.8296mL9.1480mL18.2959mL5mM0.3659mL1.8296mL3.6592mL10mM0.1830mL0.9148mL1.8296mL請根據產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?案，配制前請先配制澄的儲備液，再依次添加助溶劑(為保證實驗結果的可靠性，體內實驗的?作液，建議您現?現配，當天使?；澄的儲備液可以根據儲存條件，適當保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(3.81mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(3.81mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.81mM);Clearsolution1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemE4.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.81mM);Clearsolution5.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.81mM);Clearsolution6.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.81mM);ClearsolutionBIOLOGICALACTIVITY?物活性KB-5492anhydrous?種有效的和選擇性的sigma受體抑制劑，抑制[3H]1,3-di(2-tolyl)guanidine(DTG)與sigma受體結合，IC50值為3.15μM。KB-5492anhydrous?種抗潰瘍藥。IC50&TargetIC50:3.15μM(sigmareceptor)[1]體外研究KB-5492(0.001-100μM)inhibitsspecific[3H]DTGbindinginaconcentration-dependentmanner[1].KB-5492(0.1-1mM)significantlyandconcentration-dependentlypreventstheethanol-andacidifiedaspirin-inducedincreasesin51Crreleasefromgastricepithelialcells[2].體內研究KB-5492(200?mg/kg;p.o.)preventsmacroscopiclesionsinthegastricmucosa[2].AnimalModel:MaleSprague-Dawleyratsweighing210-240gareinducedgastricmucosaldamage[2]Dosage:200?mg/kgAdministration:OralgavageResult:Reducedthelesionlengthascomparedwiththecontrol.Preventedthedeepmucosallesionsandexfoliationofsurfaceepithelialcells.REFERENCES[1].HaradaY,et,al.ReceptorbindingprofilesofKB-5492,anovelanti-ulceragent,atsigmareceptorsinguinea-pigbrain.EurJPharmacol.1994May2;256(3):321-8.[2].MorimotoY,et,al.EffectsofKB-5492,anewanti-ulceragent,onethanol-andacidifiedaspirin-inducedgastricmucosaldamageinvivoandinvitro.JpnJPharmacol.1994Jan;64(1):41-7.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicati