LGD-6972-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemELGD-6972Cat.No.:HY-12525CASNo.:1207989-09-0分?式:C??H??N?O?S分?量:702.9作?靶點(diǎn):GCGR作?通路:GPCR/GProtein儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:125mg/mL(177.83mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.4227mL7.1134mL14.2268mL5mM0.2845mL1.4227mL2.8454mL10mM0.1423mL0.7113mL1.4227mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)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(qǐng)先按照InVitro?式配制澄的儲(chǔ)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(chǔ)備液可以根據(jù)儲(chǔ)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(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(2.96mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(2.96mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(2.96mM);ClearsolutionBIOLOGICALACTIVITY?物活性LGD-6972?種選擇性的具有?服活性的胰??糖素受體(glucagonreceptor)拮抗劑。LGD-6972可?于2型糖尿病的研究。體外研究Invitro,LGD-6972bindscompetitivelytoglucagonreceptor(GCGR)withhighaffinityandselectivity,suppressingbothcAMPandglucoseproduction[1].體內(nèi)研究Invivo,LGD-6972reducesacuteglucagon-stimulatedhyperglycaemiaaswellasthehyperglycaemiaobservedindiabeticmousemodels.ThepharmacologicalactivityofLGD-6972appearstobemediatedprimarilybyinhibitingglucagonreceptorsignaling[1].REFERENCES[1].VajdaEG,etal.PharmacokineticsandpharmacodynamicsofsingleandmultipledosesoftheglucagonreceptorantagonistLGD-6972inhealthysubjectsandsubjectswithtype2diabetesmellitus.DiabetesObesMetab.2017Jan;19(1):24-32.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-8