Linerixibat-GSK2330672-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELinerixibatCat.No.:HY-16643CASNo.:1345982-69-5Synonyms:GSK2330672分⼦式:C₂₈H₃₈N₂O₇S分⼦量:546.68作⽤靶点:ApicalSodium-DependentBileAcidTransporter作⽤通路:MembraneTransporter/IonChannel储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(91.46mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8292mL9.1461mL18.2922mL5mM0.3658mL1.8292mL3.6584mL10mM0.1829mL0.9146mL1.8292mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:2.5mg/mL(4.57mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.57mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.57mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Linerixibat(GSK2330672)⼀种⾼效，不可吸收且具有⼝服活性的顶端钠依赖性胆汁酸转运蛋⽩(ASBT)抑制剂，对⼈ASBT的IC50为42nM。Linerixibat可⽤作降脂剂，具有研究2型糖尿病和原发性胆性胆管炎的潜⼒。IC50&TargetIC50:42nM(Apicalsodium-dependentbileacidtransporter(ASBT))[1]体外研究Thezwitterionic,nonhygroscopic,crystallinesaltformofLinerixibat(Compound56)showsgoodaqueoussolubilityatpH7.4(>7mg/mL),excellentthermalstability,anddidnotgeneratereactiveorhumanspecificmetabolite,characteristics[1].体内研究Linerixibat(GSK2330672;0.05-10mg/kg;oralgavage;twicedaily;for14days;maleZDFrat)treatmentlowersglucoseinananimalmodeloftype2diabetes[1].AnimalModel:MaleZuckerDiabeticFatty(ZDF)rat[1]Dosage:0.05mg/kg,0.1mg/kg,0.5mg/kg,1mg/kg,5mg/kg,10mg/kgAdministration:Oralgavage;twicedaily;for14daysResult:Ledtoa1.30-1.64%reductioninhemoglobinA1c(HbA1c),agreaterthan50%reductioninnonfastedplasmaglucosetobelow200mg/dL,andstatisticallysignificanthigherplasmainsulin.户使⽤本产品发表的科研⽂献•NatCommun.2020Jul17;11(1):3612.•SciAdv.2021Feb3;7(6):eaaz9857.•CellMolGastroenterolHepatol.2021May6;S2352-345X(21)00084-9.•FoodFunct.2021Aug10.•CellMicrobiol.2020Jan;22(1):e13127.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].WuY,etal.Discoveryofahighlypotent,nonabsorbableapicalsodium-dependentbileacidtransporterinhibitor(GSK2330672)fortreatmentoftype2diabetes.JMedChem.2013Jun27;56(12):5094-114.[2].Linerixibat(GSK2330672)grantedOrphanStatus.September24,2019.[3].WangY,etal.HNF4αRegulatesCSADtoCoupleHepaticTaurineProductiontoBileAcidSynthesisinMice.GeneExpr.2018Aug22;18(3):187-196.McePdfHeightCaution:Producthasnotbeenfullyvalidatedf