PF-06291874-Glucagon-receptor-antagonists-4-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPF-06291874Cat.No.:HY-19947CASNo.:1393124-08-7Synonyms:Glucagonreceptorantagonists-4分⼦式:C₂₆H₂₈F₃N₃O₄分⼦量:503.51作⽤靶点:GCGR作⽤通路:GPCR/GProtein储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(198.61mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9861mL9.9303mL19.8606mL5mM0.3972mL1.9861mL3.9721mL10mM0.1986mL0.9930mL1.9861mL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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(4.13mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.13mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.13mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性PF-06291874⼀个⼝服有效的胰⾼⾎糖素受体的⾮肽类拮抗剂。PF-06291874正⽤于2型糖尿病(T2DM)的研究。体内研究PF-06291874exposureisapproximatelydose-proportionalwithahalf-lifeof-19.7-22.7h.PF-06291874hasafastonandoffrate.PF-06291874ishighlyboundtohumanplasmaprotein,withameanfreefractionof-0.55%[3].REFERENCES[1].EstherC.Y.Leeetal.Identificationofanovelconformationallyconstrainedglucagonreceptorantagonist.BioorgMedChemLett,2014Feb1,24(3):839-44.[2].DerekJNunez,etal.Glucagonreceptorasadrugtarget:Awitches'brewofeyeofnewt(peptides)andtoeoffrog(receptors).DiabetesObesMetab.2018Feb;20(2):233-237.[3].DJKazierad,etal.EffectsofmultipleascendingdosesoftheglucagonreceptorantagonistPF-06291874inpatientswithtype2diabetesmellitus.DiabetesObesMetab.2016Aug;18(8):795-802.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel