KB-5492-anhydrous-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEKB-5492anhydrousCat.No.:HY-19120CASNo.:129200-10-8分⼦式:C₂₇H₃₄N₂O₁₀分⼦量:546.57作⽤靶点:SigmaReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(457.40mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8296mL9.1480mL18.2959mL5mM0.3659mL1.8296mL3.6592mL10mM0.1830mL0.9148mL1.8296mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存⽅式和期限。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(3.81mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(3.81mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.81mM);Clearsolution1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE4.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.81mM);Clearsolution5.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.81mM);Clearsolution6.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.81mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性KB-5492anhydrous⼀种有效的和选择性的sigma受体抑制剂，抑制[3H]1,3-di(2-tolyl)guanidine(DTG)与sigma受体结合，IC50值为3.15μM。KB-5492anhydrous⼀种抗溃疡药。IC50&TargetIC50:3.15μM(sigmareceptor)[1]体外研究KB-5492(0.001-100μM)inhibitsspecific[3H]DTGbindinginaconcentration-dependentmanner[1].KB-5492(0.1-1mM)significantlyandconcentration-dependentlypreventstheethanol-andacidifiedaspirin-inducedincreasesin51Crreleasefromgastricepithelialcells[2].体内研究KB-5492(200ꢀmg/kg;p.o.)preventsmacroscopiclesionsinthegastricmucosa[2].AnimalModel:MaleSprague-Dawleyratsweighing210-240gareinducedgastricmucosaldamage[2]Dosage:200ꢀmg/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