LY2955303-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemELY2955303Cat.No.:HY-107765CASNo.:1433497-19-8分?式:C??H??N?O?分?量:578.74作?靶點(diǎn):RAR/RXR;Autophagy作?通路:MetabolicEnzyme/Protease;Autophagy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:30mg/mL(51.84mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.7279mL8.6395mL17.2789mL5mM0.3456mL1.7279mL3.4558mL10mM0.1728mL0.8639mL1.7279mL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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2mg/mL(3.46mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2mg/mL(3.46mM);ClearsolutionBIOLOGICALACTIVITY?物活性L(fǎng)Y2955303?種有效且有選擇性的視酸受體γ(RARγ)的拮抗劑，其Ki值為1.09nM。IC50&TargetKi:1.09nM(RARγ)[1]體外研究LY2955303istestedandobservedthatthebindingKisforRARα,RARβandRARγare>1700,>2980and1.09nM,respectively.ThefunctionalKiforRARγis7.1±4.9nM[1].體內(nèi)研究AsingleoraldoseofLY2955303demonstratesadoseresponsiveeffectwherebytheratreducesdifferentialweightbearing(ED50=0.72mg/kg)[1].戶(hù)使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?CellRes.2022Jun;32(6):513-529.?MediatorsInflamm.2022Nov7;2022:1875736.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].HughesNE,etal.Identificationofpotentandselectiveretinoicacidreceptorgamma(RARγ)antagonistsforthetreatmentofosteoarthritispainusingstructurebaseddrugdesign.BioorgMedChemLett.2016Jul15;26(14):3274-3277.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-8