E6130-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEE6130Cat.No.:HY-107456CASNo.:1427058-33-0分?式:C??H??ClF?N?O?分?量:556.06作?靶點(diǎn):CX3CR1作?通路:Immunology/Inflammation儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥250mg/mL(449.59mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.7984mL8.9918mL17.9837mL5mM0.3597mL1.7984mL3.5967mL10mM0.1798mL0.8992mL1.7984mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(3.74mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.74mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.74mM);ClearsolutionBIOLOGICALACTIVITY?物活性E6130?種具有?服活性的，?度選擇性的CX3CR1調(diào)節(jié)劑，有研究炎癥性腸病的潛?。IC50&TargetCX3CR1[1]體外研究E6130isanorallyactiveandhighlyselectiveCX3CR1modulator,inhibitsthefractalkine-inducedchemotaxisofhumanperipheralbloodnaturalkillercells(IC50,4.9nM),anddown-regulatesCX3CR1onthecellsurfaceofCD56+NKcellswithanEC50valueof5.2nM.E6130alsoshowsagonisticactivityviaCX3CR1withrespecttoGTPγSbinding(EC50=133nM)andβ-arrestinrecruitment(EC50=2.4μM)inCX3CR1-expressingCHO-K1membranebutshownoantagonisticactivity[1].體內(nèi)研究E6130(10or30mg/kg,p.o.)reducesseveralinflammatoryboweldisease-relatedparametersinamurineCD4+CD45RBhighT-cell-transfercolitismodelandamurineoxazolone-inducedcolitismodel[1].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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