RORγt-inverse-agonist-13-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERORγtinverseagonist13Cat.No.:HY-131338CASNo.:2170477-75-3分?式:C??H??Cl?F?N?O?分?量:513.29作?靶點(diǎn):ROR作?通路:MetabolicEnzyme/Protease儲(chǔ)存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(194.82mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.9482mL9.7411mL19.4822mL5mM0.3896mL1.9482mL3.8964mL10mM0.1948mL0.9741mL1.9482mL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>>90%cornoilSolubility:≥2.5mg/mL(4.87mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性RORγtinverseagonist13(Compound3i)有效的、具有?服活性的、選擇性的RORγt反向激動(dòng)劑，其IC50值為63.8nM。IC50&TargetROR-γ63.8nM(IC50)體外研究RORγtinverseagonist13(Compound3i)exhibitsactivitywithaninhibitionof76%at0.3?μMinTh17celldifferentiationassay[1].體內(nèi)研究RORγtinverseagonist13(Compound3i,25mg/kg,Orally,twicedaily)demonstratsexcellentinvivoPKprofileinmiceandgoodinvivoefficacyinanIMQ-inducedpsoriasismicemodel[1].AnimalModel:Imiquimod(IMQ)-inducedpsoriasismicemodel[1].Dosage:25mg/kg.Administration:Orally,twicedaily.Result:Broughtinasignificantreductioninclinicalseverityofpsoriasisasmeasuredthroughtheearerythema,backskinerythemaandscalinessscales.AnimalModel:MaleCD-1Mice[1].Dosage:1mg/kg(i.v.)and5mg/kg(p.o.)(PharmacokineticAnalysis).Administration:IVorPO,singledose.Result:Cmax:609.67ng/mL(PO),1550ng/mL(IV).T1/2:3.63h(PO),3.04h(IV).REFERENCES[1].NannanSun,etal.Discoveryofcarboxyl-containingbiarylureasaspotentRORγtinverseagonists.EurJMedChem.2020Jul5;202:112536.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Te