Safotibant-LF22-0542-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESafotibantCat.No.:HY-100827CASNo.:633698-99-4Synonyms:LF22-0542分⼦式:C₂₅H₃₄N₄O₅S分⼦量:502.63作⽤靶点:BradykininReceptor作⽤通路:GPCR/GProtein储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Safotibant(LF22-0542)激肽B1受体(BKB1R)的选择性拮抗剂，对⼈和⿏BKB1R的Ki分别为0.35和6.5nM。Safotibant在⼩⿏模型中表现出镇痛和抗炎活性[1][2]。体内研究Safotibant(10mg/kg,s.c.,3timesadayfor8days)exhibitsanalgesicpropertyagainstbonecancer-inducedpaininosteolyticsarcomaxenograftC3H/HeJmicemodel,withoutaffectingdiseaseprogression[1].Safotibant(oneeyedropapplication,twiceadayfor7days)inhibitsexpressionsofinflammatorymediatorsB1R,iNOS,IL-1β,COX-2,VEGF-R2andHIF-1α,reversesdiabetes-inducedretinalinflammationandoxidativestressinstreptozotocin(STZ)-diabeticWistarratsmodel[2].AnimalModel:OsteolyticsarcomaxenograftC3H/HeJmicemodel[1]Dosage:10mg/kgAdministration:s.c.,3timesadayfor8daysResult:Decreasednumbersofflinchingandtimespentonspontaneousguarding.AnimalModel:Streptozotocin(STZ)-diabeticWistarratsmodel[2]Dosage:OneeyedropAdministration:Oneyesapplication,twiceadayfor7days1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:Reversedretinalvascularhyperpermeability,decreasedlevelsofretinalleukostasisandsuperoxideanionin3retinalnuclearlayers.REFERENCES[1].SevcikMA,etal.,AnalgesicefficacyofbradykininB1antagonistsinamurinebonecancerpainmodel.JPain.2005Nov;6(11):771-5.[2].PouliotM,etal.,OcularapplicationofthekininB1receptorantagonistLF22-0542inhibitsretinalinflammationandoxidativestressinstreptozotocin-diabeticrats.PLoSOne.2012;7(3):e33864.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3