AZD8848-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAZD8848Cat.No.:HY-111269CASNo.:866269-28-5分?式:C??H??N?O?分?量:569.7作?靶點:Toll-likeReceptor(TLR)作?通路:Immunology/Inflammation儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:25mg/mL(43.88mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.7553mL8.7765mL17.5531mL5mM0.3511mL1.7553mL3.5106mL10mM0.1755mL0.8777mL1.7553mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(4.39mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(4.39mM);Suspendedsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.39mM);ClearsolutionBIOLOGICALACTIVITY?物活性AZD8848?種選擇性的TLR7前體藥激動劑，?于哮喘和過敏性?炎的研究[1]。IC50&TargetTLR7[1]體外研究AZD8848showsgoodactivityagainstTLR7,withcellularpEC50sof7.0and6.6forhumanTLR7andratTLR7,respectively[1].AZD8848hasanEC50of4nMintheinductionofIFNαfromhumanPBMCsandanIC50of0.2-1.0nMfortheinhibitionofIL-5,irrespectiveofwhethertheTcellshavebeenpolyclonallystimulatedwithPHAorviaantigenpresentation[1].AZD8848isapotent,selectiveTLR7agonistantedrugabletoinhibitTh2responsesinvitro[1].AZD8848hasnoactivityagainsthumanTLR8oragainstanyoftheotherhumanTLRs[1].體內(nèi)研究AZD8848(0.1-1mg/kg;intratracheal)hasagoodpharmacokineticsintheBrownNorwayrat[1].AZD8848(0.3mg/kg;Intratracheal)suppressestheovalbumin(OVA)challengeintheratallergymodel[1].AnimalModel:BrownNorwayratallergymodel[1]Dosage:0.1mg/kg,1mg/kgAdministration:Intratracheal(24hourspriortoand24hoursaftertheOVAchallenge)Result:SuppressedOVAchallengeinadose-dependentmanner.AnimalModel:BrownNorwayrat[1]Dosage:0.3mg/kg(PharmacokineticAnalysis)Administration:IntratrachealResult:Hasaveryshorthalf-life(0.2min)inratbloodanddeclinedslowlyafterthispointandlevelsabove1000nmol/kgweremaintainedforover5hours.REFERENCES[1].DelaneyS,etal.TolerabilityinmanfollowinginhalationdosingoftheselectiveTLR7agonist,AZD8848.BMJOpenRespirRes.2016Feb23;3(1):e000113.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalap