E6130-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEE6130Cat.No.:HY-107456CASNo.:1427058-33-0分⼦式:C₂₈H₃₇ClF₃N₃O₃分⼦量:556.06作⽤靶点:CX3CR1作⽤通路:Immunology/Inflammation储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥250mg/mL(449.59mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.7984mL8.9918mL17.9837mL5mM0.3597mL1.7984mL3.5967mL10mM0.1798mL0.8992mL1.7984mL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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(3.74mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.74mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.74mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性E6130⼀种具有⼝服活性的，⾼度选择性的CX3CR1调节剂，有研究炎症性肠病的潜⼒。IC50&TargetCX3CR1[1]体外研究E6130isanorallyactiveandhighlyselectiveCX3CR1modulator,inhibitsthefractalkine-inducedchemotaxisofhumanperipheralbloodnaturalkillercells(IC50,4.9nM),anddown-regulatesCX3CR1onthecellsurfaceofCD56+NKcellswithanEC50valueof5.2nM.E6130alsoshowsagonisticactivityviaCX3CR1withrespecttoGTPγSbinding(EC50=133nM)andβ-arrestinrecruitment(EC50=2.4μM)inCX3CR1-expressingCHO-K1membranebutshownoantagonisticactivity[1].体内研究E6130(10or30mg/kg,p.o.)reducesseveralinflammatoryboweldisease-relatedparametersinamurineCD4+CD45RBhighT-cell-transfercolitismodelandamurineoxazolone-inducedcolitismodel[1].户使⽤本产品发表的科研⽂献•Cancers(Basel).2022,14(1),64.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].WakitaH,etal.E6130,aNovelCX3CChemokineReceptor1(CX3CR1)Modulator,AttenuatesMucosalInflammationandReducesCX3CR1+LeukocyteTraffickinginMicewithColitis.MolPharmacol.2017Nov;92(5):502-509.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch