Carotegrast-methyl-AJM300-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECarotegrastmethylCat.No.:HY-124290CASNo.:401905-67-7Synonyms:AJM300分?式:C??H??Cl?N?O?分?量:569.44作?靶點:Integrin作?通路:Cytoskeleton儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(175.61mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.7561mL8.7806mL17.5611mL5mM0.3512mL1.7561mL3.5122mL10mM0.1756mL0.8781mL1.7561mL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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:1.25mg/mL(2.20mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:1.25mg/mL(2.20mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Carotegrastmethyl(AJM300)?種?服有效和選擇性α4整聯(lián)蛋?(α4integrin)拮抗劑。HCA2969是Carotegrastmethyl的活性代謝產(chǎn)物，?種特異的雙重α4β1/α4β7整聯(lián)蛋?拮抗劑。Carotegrastmethyl可預(yù)防??結(jié)腸炎。體外研究HCA2969inhibitshumanα4β1integrin(KD=0.32nM;IC50=5.8nM),humanα4β7integrin(KD=0.46nM;IC50=1.4nM)andmouseα4β7integrin(KD=0.2nM;IC50=26nM)inJurkat,RPMI-8866andTK-1celllines[1].體內(nèi)研究Carotegrastmethyl(AJM300;oral;0.03-1%;for15days)preventsthedevelopmentofcolitisinducedbytransferofIL-10deficientCD4+Tcellsinmice[1].Carotegrastmethyl(oral;0.3,3,30,or30mg/kg;asingleoral)inhibitsLymphocytehomingtoPeyer'spatchesandincreasesperipherallymphocytecountsinadose-dependentmannerinBALB/cmice(8weeksofage,female)[1].AnimalModel:MousemodelofcolitisinducedbyadoptivetransferofIL-10deficientCD4+Tcells[1]Dosage:Diet;0.03,0.1,0.3or1%Administration:For15daysResult:Hadahistologicalimprovementinepithelialcellhyperplasia,reducedinflammatorycellinfiltrationandadecreaseinmucusproduction.PreventedanincreaseinthecolonweightinamodelofcolitisinducedbyadoptivetransferofCD4+CD45RBhighTcells.REFERENCES[1].ToshihikoSugiura,etal.Oraltreatmentwithanovelsmallmoleculealpha4integrinantagonist,AJM300,preventsthedevelopmentofexperimentalcolitisinmice.JCrohnsColitis.2013Dec;7(11):e533-42.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.