RF9-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERF9Cat.No.:HY-107382CASNo.:876310-60-0分?式:C??H??N?O?分?量:482.62作?靶點(diǎn):NeuropeptideYReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲(chǔ)存?式:Sealedstorage,awayfrommoisturePowder-80°C2years-20°C1yearInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:125mg/mL(259.00mM;Needultrasonic)H2O:16.67mg/mL(34.54mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.0720mL10.3601mL20.7202mL5mM0.4144mL2.0720mL4.1440mL10mM0.2072mL1.0360mL2.0720mL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,awayfrommoisture)。-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)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.31mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.31mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.31mM);ClearsolutionBIOLOGICALACTIVITY?物活性RF9?種有效且有選擇性的神經(jīng)肽FF受體(NeuropeptideFFreceptor)拮抗劑，對(duì)于hNPFF1R和hNPFF2R的Ki值分別為58和7nM。IC50&TargethNPFF1RhNPFF2R58nM(Ki)75nM(Ki)體外研究RF9(10μM)pretrementcompletelyblocksNPFFinducedneuriteoutgrowthofNeuro2Acells[2].體內(nèi)研究RF9(0.1mg/kg,s.c.)withheroincoadministrationpreventsheroin-induceddelayedhyperalgesiaandtolerance[1].RF9(10μg)infusedalonedoesnotresultinasignificantalterationofMAPorheartrate.Conversely,MAPandheartrateincreasesevokedbyNPFFaresignificantlyblockedwhenNPFFisappliedinconjunctionwithRF9[1].AnimalModel:Rats[1].Dosage:0.1mg/kg.Administration:S.C.30minbefore0.3mg/kgheroinorsalineonbasalnociceptivethresholdinrats.Result:Opposedtodelayeheroin-inducedhyperalgesiaandassociatedtolerance.REFERENCES[1].SimoninF,etal.RF9,apotentandselectiveneuropeptideFFreceptorantagonist,preventsopioid-inducedtoleranceassociatedwithhyperalgesia.ProcNatlAcadSciUSA.2006Jan10;103(2):466-71.[2].TingZhang,etal.DiscoveryofTwoNovelBranchedPeptidomimeticsContainingendomorphin-2andRF9Pharmacophores:SynthesisandNeuropharmacologicalEvaluation.BioorgMedChem.2019Feb15;27(4):630-643.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.