BMS-986278-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBMS-986278Cat.No.:HY-139853CASNo.:2170126-74-4分⼦式:C₂₂H₃₁N₅O₅分⼦量:445.51作⽤靶点:LPLReceptor作⽤通路:GPCR/GProtein储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(224.46mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2446mL11.2231mL22.4462mL5mM0.4489mL2.2446mL4.4892mL10mM0.2245mL1.1223mL2.2446mL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>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(5.61mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.61mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.61mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性BMS-986278⼀种有效和具有⼝服活性的⾎磷脂酸受体1(LPA1)拮抗剂，对⼈和⼩⿏LPA1的Kb值分别为6.9nM和4.0nM。BMS-986278可⽤于研究肺纤维化疾病。IC50&TargetKb:6.9nM(humanLPA1),4.0nM(mouseLPA1)[1]体外研究BMS-986278isahigh-affinityLPA1antagonist,withKbsof6.9nMand4.0nMforhumanandmouseLPA1inCHOcellsoverexpressingLPA1[1].BMS-986278antagonizesLysophosphatidicacid(LPA)-stimulatedcalciumfluxinnormalhumanlungfibroblasts,withaKbof5.8nM[1].体内研究BMS-986278(0.1-10mg/kg;asinglep.o.)completelyinhibitsLPA-stimulatedsystemichistaminereleaseinaconcentration-dependentmannerinCD1mice[1].BMS-986278(3-30mg/kg;p.o.twicedailyfor14d)decreasesBleomycin-inducedcollagendeposition/lungfibrosisinrats[1].PharmacokineticsofBMS-986278inpreclinicalspecies[1]plasmaclearance((mL/min)/kg)Vss(L/kg)oralbioavailability(%)T1/2(h)plasmaproteinbinding(%free)mouse375.5702.531.4rat153.51004.512.6monkey2.01.679110.8AnimalModel:MaleSprague-Dawleyrats(10weeks)wereadministeredBleomycin[1]Dosage:3,10,and30mg/kgAdministration:P.o.twicedailyfor14daysResult:Resultedinsignificantdecreasesinthelungsectionpercentfibroticareaforthe3mg/kg(48%)and10mg/kg(56%)dosegroups.REFERENCES[1].ChengPTW,et,al.DiscoveryofanOxycyclohexylAcidLysophosphatidicAcidReceptor1(LPA1)AntagonistBMS-986278fortheTreatmentofPulmonaryFibroticDiseases.JMedChem.2021Nov11;64(21):15549-15581.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicat