Etalocib-LY293111-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEEtalocibCat.No.:HY-13628CASNo.:161172-51-6Synonyms:LY293111;VML295分⼦式:C₃₃H₃₃FO₆分⼦量:544.61作⽤靶点:LeukotrieneReceptor;Apoptosis作⽤通路:GPCR/GProtein;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(183.62mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8362mL9.1809mL18.3618mL5mM0.3672mL1.8362mL3.6724mL10mM0.1836mL0.9181mL1.8362mL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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。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。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:2.5mg/mL(4.59mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.59mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Etalocib(LY293111)具有⼝服活性的⽩三烯(LTB4)受体的拮抗剂，抑制[3H]LTB4结合的Ki值为25nM.Etalocib(LY293111)抑制LTB4诱导的钙动员的lC50值为20nM。Etalocib(LY293111)可诱导凋亡。体外研究Etalocib(LY293111)elicitsaconcentration-dependentinhibitionofLTB4inducedCD11bup-regulation[1].Etalocib(LY293111)isanextremelypotentandselectiveantagonistofhumanneutrophilfunctioninvitro[2].Etalocib(LY293111,250and500nM,24-72h)inducesapoptosisandinhibitsproliferationinhumanpancreaticcancercells[3].CellProliferationAssay[3]CellLine:MiaPaCa-2andAsPC-1humanpancreaticcancercells.[3]Concentration:500nM.IncubationTime:24,48,and72h.Result:Causedbothaconcentration-dependentandtime-dependentinhibitionofthymidineincorporationinbothMiaPaCa-2andAsPC-1humanpancreaticcancercells.ApoptosisAnalysis[3]CellLine:MiaPaCa-2andAsPC-1humanpancreaticcancercells.Concentration:250and500nM.IncubationTime:24h.Result:Inducedapoptosisinhumanpancreaticcancercells.体内研究Etalocib(LY293111)producesadose-relatedinhibitionofacuteleukotrieneB4-inducedairwayobstructionwhenadministeredi.v.(ED50=14µg/kg)orp.o.(ED50=0.4mg/kg)[2].Etalocib(LY293111,10mg/kg)inhibitsA23187-inducedlunginflammatorychangesat1h[2].Etalocib(LY293111,250mg/kg/day,orally)inhibitsgrowthofhumanpancreaticcancerxenograftsinathymicmice[3].AnimalModel:Guineapigs[2].Dosage:1-10mg/kg.Administration:Orallyonce.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:Asingle1mg/kgoraldoseinhibitedexcisedlunggasvolumeincreasesby76.7±7.1%(n=4,P4challenge,and28.6±20.3%(n=4,NS)whengiven24hbeforechallenge.Hadnoeffect(10mg/kg)onpulmonarygastrappingat1hor2hafterA23187challenge.However,at4h,thepulmonarygastrappingresponsewassignificantlylessthanthatofvehicle-treatedcontrolsandnotdifferentfromshamvalues.The10mg/kgdoseinhibitedA23187-inducedlunginflammatorychangesat1h,butwaswithouteffectat2hor4hafterchallenge.REFERENCES[1].PMarder,etal.BlockadeofHumanNeutrophilActivationby2-[2-propyl-3-[3-[2-ethyl-4-(4-fluorophenyl)-5-Hydroxyphenoxy]propoxy]phenoxy]benzoicAcid(LY293111),aNovelLeukotrieneB4ReceptorAntagonist.BiochemPharmacol.1995May26;49(11):1683-90.[2].SASilbaugh,etal.PharmacologicActionsoftheSecondGenerationLeukotrieneB4ReceptorAntagonistLY29311:InVivoPulmonaryStudies.NaunynSchmiedebergsArchPharmacol.2000Apr;361(4):397-404.[3].Wei-GangTong,etal.LeukotrieneB4ReceptorAntagonistLY293111InhibitsProliferationandInducesApoptosisinHumanPancreaticCancerCells.ClinCancerRes.2002Oct;8(10):3232-42.McePdfHeightCautio