AS-041164-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAS-041164Cat.No.:HY-118521CASNo.:6318-41-8分⼦式:C₁₁H₇NO₄S分⼦量:249.24作⽤靶点:PI3K作⽤通路:PI3K/Akt/mTOR储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:125mg/mL(501.52mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM4.0122mL20.0610mL40.1220mL5mM0.8024mL4.0122mL8.0244mL10mM0.4012mL2.0061mL4.0122mL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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。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：10%DMSO>>90%cornoilSolubility:≥1.47mg/mL(5.90mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性AS-041164⼀种有效的，选择性的，具有⼝服活性的PI3Kγ亚型抑制剂，IC50为70nM。AS-041164对PI3Kα，PI3Kβ和PI3Kδ的活性较低(IC50分别为240nM，1.45μM和1.70μM)。AS-041164具有抗炎作⽤。IC50&TargetPI3KγPI3KαPI3KβPI3Kδ70nM(IC50)240nM(IC50)1.4μM(IC50)1.7μM(IC50)体内研究AS-041164(10-100mg/kg;oraladministration;once)treatmentresultsinthereductionofinflammatoryswellinginthemodelofcarrageenan-inducedpawedema[1].AS-041164(3-100mg/kgp.o.)treatmentdose-dependentlydecreasesr-hregulatedonactivationnormalTcellexpressedandsecreted(RANTES)-inducedneutrophilrecruitmentinmice.TheED50valueforAS-041164is27.35mg/kg.AS-041164blocksRANTES-inducedchemotaxisandreducesthelevelofAKTphosphorylation[1].AnimalModel:MaleWistarrats(100-150g)injectedwithcarrageenan[1]Dosage:10mg/kg,30mg/kg,100mg/kgAdministration:Oraladministration;onceResult:Inducedasignificantreductionofpawthickness.REFERENCES[1].ChiaraFerrandi,etal.Phosphoinositide3-kinasegammainhibitionplaysacrucialroleinearlystepsofinflammationbyblockingneutrophilrecruitment.JPharmacolExpTher.2007Sep;322(3):923-30.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly