PF-06291874-Glucagon-receptor-antagonists-4-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPF-06291874Cat.No.:HY-19947CASNo.:1393124-08-7Synonyms:Glucagonreceptorantagonists-4分?式:C??H??F?N?O?分?量:503.51作?靶點(diǎn):GCGR作?通路:GPCR/GProtein儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(198.61mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.9861mL9.9303mL19.8606mL5mM0.3972mL1.9861mL3.9721mL10mM0.1986mL0.9930mL1.9861mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(4.13mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.13mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.13mM);ClearsolutionBIOLOGICALACTIVITY?物活性PF-06291874?個(gè)?服有效的胰??糖素受體的?肽類拮抗劑。PF-06291874正?于2型糖尿病(T2DM)的研究。體內(nèi)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