Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECintirorgonCat.No.:HY-104037CASNo.:2055536-64-4Synonyms:LYC-55716分?式:C??H??F?NO?S分?量:603.53作?靶點(diǎn):ROR作?通路:MetabolicEnzyme/Protease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:≥113.3mg/mL(187.73mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.6569mL8.2846mL16.5692mL5mM0.3314mL1.6569mL3.3138mL10mM0.1657mL0.8285mL1.6569mL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)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請(qǐng)依序添加每種溶劑：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(4.14mM);ClearsolutionBIOLOGICALACTIVITY?物活性Cintirorgon(LYC-55716)?種?創(chuàng)的、選擇性的，具有?服活性的RORγ激動(dòng)劑。Cintirorgon(LYC-55716)調(diào)節(jié)RORγ表達(dá)的T淋巴細(xì)胞免疫細(xì)胞的因表達(dá)，增強(qiáng)效應(yīng)?功能，降低免疫抑制，降低腫瘤?長，提??存率[1][2]。IC50&TargetRORγ[1]體內(nèi)研究UponoraladministrationofRORγagonistCintirorgon(LYC-55716),thisagentselectivelybindstothenuclearreceptortranscriptionfactorRORγ,formingareceptorcomplexthattranslocatestothenucleus,andbindstoRORresponseelements(ROREs),enhancingthefunction,proliferationandsurvivaloftype17Tcells,includingTh17(helperTcells)andTc17(cytotoxicTcells).RORγ,thenuclearreceptortranscriptionfactorthatisinvolvedinTh17/Tc17differentiation,playsakeyroleinimmuneactivation.Cintirorgon(LYC-55716)isalsoorallybioavailable,whilethenewgenerationofimmuno-oncologydrugs-ncludingPD-1/PD-L1inhibitorsaredeliveredbyinjection[1].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?PharmacolRes.2021Jul30;105793.?EurJMedChem.2021,113585.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LyceraAnnouncesInitiationofPhase1/2aStudyARGONofImmuno-OncologyCandidateLYC-55716inPatientswithAdvancedSolidTumors.Jan04,2017.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseo