Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBB-Cl-AmidineCat.No.:HY-111347CASNo.:1802637-39-3分?式:C??H??ClN?O分?量:459.97作?靶點(diǎn):ProteinArginineDeiminase作?通路:Epigenetics儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:125mg/mL(271.76mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.1741mL10.8703mL21.7405mL5mM0.4348mL2.1741mL4.3481mL10mM0.2174mL1.0870mL2.1741mL體內(nèi)實(shí)驗(yàn)請根據(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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.52mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.52mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.52mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性BB-Cl-Amidine肽精氨酸脫胺酶(PAD)的抑制劑。IC50&TargetPAD[1].體內(nèi)研究TreatmentwithBB-Cl-amidinesubtlyreducessplenomegalyinMRL/lprmice,whilethereisatrendtowardsincreasedcirculatinglevelsofanti-NETantibodieswithPADinhibitortreatment.However,neitherPADinhibitoraffectedbodyweightortotalIgGlevels.Indeed,treatmentwithbothCl-amidineandBB-Cl-amidinesignificantlyimprovesendothelium-dependentvasorelaxation.TheBB-Cl-amidinegroupalsoshowsastrongtrendtowardsdownregulationofIRGs.TreatmentwitheitherCl-amidineorBB-Cl-amidinesignificantlyimprovesmuzzlealopecia,inmanycasespreventingitentirely[1].AnimalModel:MRL/lprmice[1].Dosage:1mg/kg.Administration:Subcutaneousinjectiondailyfrom8to14weeksofage.Result:Significantlyimprovedendothelium-dependentvasorelaxationandshowedastrongtrendtowardsdownregulationofIRGs.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?NatCellBiol.2021Oct6.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].KnightJS,etal.PeptidylargininedeiminaseinhibitiondisruptsNETformationandprotectsagainstkidney,skinandvasculardiseaseinlupus-proneMRL/lprmice.AnnRheumDis.2015Dec;74(12):2199-206.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch