Emodin-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEEmodinCat.No.:HY-14393CASNo.:518-82-1分⼦式:C₁₅H₁₀O₅分⼦量:270.24作⽤靶点:SARS-CoV;CaseinKinase;Autophagy作⽤通路:Anti-infection;CellCycle/DNADamage;StemCell/Wnt;Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验Acetone:10.87mg/mL(40.22mM;Needultrasonic)扫描⼆维码，DMSO:5.41mg/mL(20.02mM;Needultrasonic)运⽤溶解⽅案计算器Ethanol:<1mg/mL(ultrasonic)(insoluble)获得适合您实验体系的溶解⽅案H2O:<0.1mg/mL(insoluble)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.7004mL18.5021mL37.0041mL5mM0.7401mL3.7004mL7.4008mL10mM0.3700mL1.8502mL3.7004mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存⽅式和期限。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶1.请依序添加每种溶剂：0.5%MC0.5%Tween-802.Solubility:10mg/mL(37.00mM);Suspendedsolution;Needultrasonic请依序添加每种溶剂：10%DMSO90%(20%SBE-β-CDinsaline)Solubility:1.25mg/mL(4.63mM);Suspendedsolution;Needultrasonic1/4www.MedChemEwww.MedChemE此⽅案可获得1.25mg/mL(4.63mM)的均匀悬浊液，悬浊液可⽤于⼝服和腹腔注射。以1mL⼯作液为例，取100μL12.5mg/mL的澄DMSO储备液加到900μL20%的SBE-β-CD⽣理盐⽔⽔溶3.液中，混合均匀。请依序添加每种溶剂：10%DMSO90%cornoilSolubility:≥1.25mg/mL(4.63mM);Clearsolution此⽅案可获得≥1.25mg/mL(4.63mM，饱和度未知)的澄溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。以1mL⼯作液为例，取100μL12.5mg/mL的澄DMSO储备液加到900μL⽟⽶油中，混合均匀。BIOLOGICALACTIVITY⽣物活性Emodin(Frangulaemodin)从植物⼤属中分离出来的⼀种蒽醌衍⽣物，⼀种抗SARS-CoV化合物。Emodin阻断SARS冠状病毒刺突蛋⽩和⾎管紧张素转化酶2(ACE2)的相互作⽤[1]。Emodin抑制酪蛋⽩激酶2(CK2)。具有抗炎和抗癌作⽤[2]。Emodin还⼀种有效的选择性11β-HSD1抑制剂，对⼈和⼩⿏11β-HSD1的IC50分别为186和86nM。Emodin可改饮⾷诱导的肥胖⼩⿏的代谢紊乱[3]。IC50&TargetSARS-CoVCK2αWild-typeCK2αWild-typemouse11β-HSD11.4μM(IC50,atATP5.9μM(IC50,atATP86nM(IC50)concentrationis10μconcentrationis50μM)M)human11β-HSD1186nM(IC50)体外研究Emodin(10-400μM)blocksthebindingofSproteintoACE2inadose-dependentmannerwiththeIC50valueof200μM[1].Emodin(5-50μM)inhibitstheSprotein-pseudotypedretrovirusinfectivityinadose-dependentmanner.EmodinblockstheSARS-CoVSproteinbindingtoVeroE6cells[1].Emodininhibitscaseinkinase-2(CK2)withIC50sof5.9,30.0,and7.1μMforCK2αWild-type,Ile174Alamutant,andHis160AlamutantatATPconcentrationis50μM,respectively.TheIC50sare1.40and38.00μMforCK2αWild-type,andVal66AlamutantatATPconcentrationis10μM[2].Emodinexhibitslowinhibitoryactivityagainstmouseandhuman11β-hydroxysteroiddehydrogenasetype2(11β-HSD2),withanIC50higherthan1mM,indicatingthatEmodinismorethan5000-foldselectiveforthehumanandmouse11β-HSD1enzymesoverthetype2isoenzyme[3].CellViabilityAssay[1]CellLine:VeroE6cellstransfectedwiththeplasmidencodingACE2Concentration:0,5,25,50μMIncubationTime:24hoursResult:Verocellstreatedwith50μMremained82.4±3.8%viability,theanti-SARS-CoVactivitywasnotduetotoxicity.2/4www.MedChemEwww.MedChemE体内研究Emodin(singleoraladministrationof100or200mg/kg)inhibits11β-HSD1activityinnormalC57BL/6Jmalemice[3].Emodin(100mg/kg;oraladministration;b.i.d.)improvesinsulinsensitivityandlipidmetabolism,andlowersbloodglucoseandhepaticPEPCK,andglucose-6-phosphatasemRNAindiet-inducedobese(DIO)mice[3].AnimalModel:C57BL/6Jmalemice[3]Dosage:100or200mg/kgAdministration:Acuteadministeredp.o.;Twohourslater,themicewerekilledbycervicaldislocation,Result:Significantlyinhibitedliver11β-HSD1enzymaticactivityby17.6and31.3%andmesentericfat11β-HSD1enzymaticactivityby21.5and46.7%at100or200mg/kg,respectively.AnimalModel:DIOmice(C57BL/6Jmalemicewerefedaformulatedresearchdiet)[3]Dosage:100mg/kgAdministration:Oralgavage;twiceperday;for35daysResult:Reducedfastingglucoseconcentrationsto77.2%ofthevehiclecontrolmiceafter7daysoftreatment,andtheseremainedsignificantlylowerthroughoutthetreatmentperiod.Exhibitedasignificantreductioninbloodglucoselevelsatalltime-pointsfollowingoralglucosechallengeafter24daysoftreatment.Evokedasignificantlygreaterreductioninbloodglucosevalues40and90minafterinsulininjectionafter28daysoftreatment.Theseruminsulinlevelwasalsosignificantlyreduced,to66.2%ofcontrolmice,after35daysoftreatment.Improvedthelipidprofiles.Theserumtriglycerideandtotalcholesterollevelsweresignificantlyreducedby19.3and12.5%after35daysoftreatment,respectively.Causeda22.7%reductionofnon-esterifiedfreefattyacid(NEFA)level.Loweredbodyweightandappetitefromday18ofthetreatment;theirbodyweightswerereducedby13.9%attheendoftreatment.户使⽤本产品发表的科研⽂献•NucleicAcidsRes.2021Jan8;49(D1):D1113-D1121.•ActaPharmacolSin.2021Jan;42(1):108-114.•IntImmunopharmacol.2020Dec23;91:107277.•IntImmunopharmacol.2020Nov;88:107020.•ExpCellRes.2020Aug1;393(1):112054.Seemorecustomervalidationsonwww.MedChemE3/4www.MedChemEwww.MedChemEREFERENCES[1].Tin-YunHo,etal.EmodinblockstheSARScoronavirusspikeproteinandangiotensin-convertingenzyme2interaction.AntiviralRes.2007May;74(2):92-101.[2].YingFeng,etal.Emodin,anaturalproduct,selectivelyinhibits11beta-hydroxysteroiddehydrogenasetype1andamelioratesmetabolicdisorderindiet-inducedobesemice.BrJPharmacol.2010Sep;161(1):113-26.[3].StefaniaSarno,etal.Towardtherationaldesignofproteinkinasecaseinkinase-2inhibitors.PharmacolTher.Feb-Mar2002;93(2