GS-6201-CVT-6883-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGS-6201Cat.No.:HY-10081CASNo.:752222-83-6Synonyms:CVT-6883分⼦式:C₂₁H₂₁F₃N₆O₂分⼦量:446.43作⽤靶点:AdenosineReceptor作⽤通路:GPCR/GProtein储存⽅式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:20mg/mL(44.80mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2400mL11.2000mL22.3999mL5mM0.4480mL2.2400mL4.4800mL10mM0.2240mL1.1200mL2.2400mL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。-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>>40%PEG300>>5%Tween-80>>45%salineSolubility:2mg/mL(4.48mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2mg/mL(4.48mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性GS-6201(CVT-6883)⼀种选择性的腺苷A2B受体拮抗剂。GS-6201对⼈腺苷A2B受体具有⾼亲和⼒和选择性(Ki=22nM)。GS-6201降低了⼩⿏急性⼼肌梗死(AMI)后⼼脏中caspase-1的活性，并减弱了⼼脏重塑。GS-6201减弱了致敏⼩⿏NECA，AMP或变应原诱导的⽓道反应性。IC50&TargetKi:22nM(humanA2Breceptors),1070nM(humanA3receptors),1940nM(humanA1receptors),3280nM(humanA2Areceptors)[1]体内研究GS-6201(CVT-6883)(4mg/kg;i.p.;every12hfor14days)significantlyreducesIL-6,TNF-α,E-selectin,ICAM-1,andVCAMplasmalevels[2].GS-6201(4mg/kg;i.p.;every12hfor14days)leadstoasignificantattenuationofleftandrightventricularenlargementanddysfunctionat7days,whichwasmaintainedat14daysandalsoat28days[2].GS-6201(2mg/kg;p.o.)treatmentshowstheCmax,dAUCandt1/2are1110ng/mL,6500ngh/mL,and4.25hours,respectively[1].AnimalModel:Adultout-bredmaleCD1mice(8-12weeksofage,AMImodel)[2]Dosage:4mg/kgAdministration:i.p.;every12hfor14daysResult:SignificantlyreducedIL-6,TNF-α,E-selectin,ICAM-1,andVCAMplasmalevels.AnimalModel:Sprague-Dawleyrats[1]Dosage:2mg/kgAdministration:p.o.(PharmacokineticAnalysis)Result:TheCmax,dAUCandt1/2were1110ng/mL,6500ngh/mL,and4.25hours,respectively.REFERENCES[1].ElzeinE,etal.DiscoveryofanovelA2Badenosinereceptorantagonistasaclinicalcandidateforchronicinflammatoryairwaydiseases.JMedChem.2008Apr10;51(7):2267-78.[2].ToldoS,etal.GS-6201,aselectiveblockeroftheA2Badenosinereceptor,attenuatescardiacremodelingafteracutemyocardialinfarctioninthemouse.JPharmacolExpTher.2012Dec;343(3):587-95.[3].MustafaSJ,etal.EffectofaspecificandselectiveA(2B)adenosinereceptorantagonistonadenosineagonistAMPandallergen-inducedairwayresponsivenessandcellularinfluxinamousemodelofasthma.JPharmacolExpTher.2007Mar;320(3):1246-51.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedf