BIBP3226-TFA-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBIBP3226TFACat.No.:HY-107726CASNo.:1068148-47-9分?式:C??H??F?N?O?分?量:587.59作?靶點(diǎn):NeuropeptideYReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲(chǔ)存?式:polypeptide,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(polypeptide,

sealedstorage,awayfrommoistureandlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:250mg/mL(425.47mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.7019mL8.5093mL17.0187mL5mM0.3404mL1.7019mL3.4037mL10mM0.1702mL0.8509mL1.7019mL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(sealedstorage,awayfrommoistureandlight)。-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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)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(3.54mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.54mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.54mM);ClearsolutionBIOLOGICALACTIVITY?物活性BIBP3226TFA?種有效選擇性的神經(jīng)肽YY1(NPYY1)和神經(jīng)肽FF(NPFF)受體拮抗劑，對(duì)rNPYY1，hNPFF2，rNPFF的Ki分別為1.1、79、108nM。BIBP3226TFA具有焦慮樣作?。IC50&TargetrNPYY1receptorhNPFF2rNPFF1.1nM(Ki)79nM(Ki)108nM(Ki)體內(nèi)研究BIBP3226(0.5,5μg;i.c.v.)inducesananxiogenic-likeeffectatthehigherdose[1].AnimalModel:MaleWistarrats270-350g[1]Dosage:0.5,5μgAdministration:I.c.vResult:Atthedoseof5μgcausedananxiogenic-likeeffectwhilethelowerdosewasineffective.REFERENCES[1].MollereauC,etal.AgonistandantagonistactivitiesonhumanNPFF(2)receptorsoftheNPYligandsGR231118andBIBP3226.BrJPharmacol.2001May;133(1):1-4.[2].KaskA,etal.Anxiogenic-likeeffectoftheneuropeptideYY1receptorantagonistBIBP3226:antagonismwithdiazepam.EurJPharmacol.1996Dec19;317(2-3):R3-4.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseon