CLP-3094-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECLP-3094Cat.No.:HY-141487CASNo.:312749-73-8分⼦式:C₁₅H₁₃ClN₂OS分⼦量:304.79作⽤靶点:AndrogenReceptor作⽤通路:Others储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(328.09mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.2809mL16.4047mL32.8095mL5mM0.6562mL3.2809mL6.5619mL10mM0.3281mL1.6405mL3.2809mL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:≥2.5mg/mL(8.20mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(8.20mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性CLP-3094⼀种有效的雄激素受体(AR)BF3(bindingfunction3)抑制剂。BF3-IN-1抑制AR转录活性(IC50=4μM)。CLP-3094⼀种选择性、有效的GPR142拮抗剂。体外研究CLP-3094inhibitsbothanincreaseofintracellularCa2+concentration([Ca2+]i)inducedbyL-tryptophanusingCHO-K1cellsexpressingGPR142intheaequorinassay,andanaccumulationofinositolphosphatesusingHEK293cellsexpressingGPR142intheSPAassay.TheIC50ofCLP-3094is0.2μMagainst200μML-tryptophanforthemousereceptorand2.3μMagainst1mML-tryptophanforthehumanreceptorintheaequorinassay.CLP-3094alsoinhibitstheinsulinsecretionfromisletsinducedbybothL-tryptophanandGPR142agonists[2].体内研究CLP-3094(30,100mg/kg;i.p.dailyfromDay0toDay11)consistentlydisplayedsig-nificantlylowerseverityofarthritisscoresthanvehicletreatedmice[2].AnimalModel:CAIAmousemodel(FemaleDBA1/Jmicewerei.v.administeredwith2mgofanti-collagenantibody,followedbyi.p.administrationof50μgofLPS)[2]Dosage:30,100mg/kgAdministration:I.p.dailyfromDay0toDay11Result:Dose-dependentlyreduced,bynotmuch,thearth-ritisscores.REFERENCES[1].MunugantiRS,etal.Targetingthebindingfunction3(BF3)siteoftheandrogenreceptorthroughvirtualscreening.2.developmentof2-((2-phenoxyethyl)thio)-1H-benzimidazolederivatives.JMedChem.2013;56(3):1136-1148.[2].MurakoshiM,etal.DiscoveryandpharmacologicaleffectsofanovelGPR142antagonist.JReceptSignalTransductRes.2017;37(3):290-296.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications