Vibegron-MK-4618-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEVibegronCat.No.:HY-19933CASNo.:1190389-15-1Synonyms:MK-4618分?式:C??H??N?O?分?量:444.53作?靶點(diǎn):AdrenergicReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲(chǔ)存?式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性數(shù)據(jù)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:≥4.75mg/mL(10.69mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:4.75mg/mL(10.69mM);Clearsolution;Needultrasonic3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥4.75mg/mL(10.69mM);ClearsolutionBIOLOGICALACTIVITY?物活性Vibegron(MK-4618)?種有效的，?選擇性的β3-adrenoceptor激動(dòng)劑(EC50=1.1nM)。Vibegron可?于膀胱過(guò)度活動(dòng)相關(guān)的嚴(yán)重急癥尿失禁[1][2][3]。IC50&Targetβ3adrenoceptor1.1nM(EC50)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE體內(nèi)研究Vibegron(1~12μΜ;i.v.)exhibitsdosedependentdecreasesinmicturitionpressureandincreasesinfunctionalbladdercapacity[3].Vibegron(30mg/kg;p.o.;4weeks)upregulatesmRNAlevelsoftype1,type3collagen,TGF‐β1,andHIF‐1α[4].Vibegron(1and10mg/kg;i.v.;interval30minutes)(10mg/kg)inoxo-M-treatedratsmakesbladdercapacitysignificantlydecreasedcomparedwithoxo-M-nottreatedrats(intravesicalinstillationofvehicle)[5].AnimalModel:RatDosage:1~12μΜAdministration:I.v.Result:Exhibiteddosedependentdecreasesinmicturitionpressureandincreasesinfunctionalbladdercapacity.AnimalModel:FemaleC57BL/6Nmice(9weeksold)Dosage:30mg/kgAdministration:P.o.;4weeksResult:UpregulatedmRNAlevelsoftype1,type3collagen,TGF‐β1,Caution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.andHIF‐1αat4weeks.Tel:400-820-3792ax-mail:tech@MedChemE

AnimalModel:FemaleF344rats(120–160g)Dosage:1and10mg/kgAdministration:I.v.;Interval30minutesResult:Vibegron(10mg/kg)inoxo-M-treatedratsmadebladdercapacitysignificantlydecreasedcomparedwithoxo-M-nottreatedrats(intravesicalinstillationofvehicle).REFERENCES[1].YoshidaM,etal.Efficacyofvibegron,anovelβ3-adrenoreceptoragonist,onsevereurgencyurinaryincontinencerelatedtooveractivebladder:posthocanalysisofarandomized,placebo-controlled,double-blind,comparativephase3study.BJUInt.2020;125(5):709-717.[2].YoshidaM,etal.Efficacyofnovelβ3-adrenoreceptoragonistvibegrononnocturiainpatientswithoveractivebladder:Apost-hocanalysisofarandomized,double-blind,placebo-controlledphase3study.IntJUrol.2019;26(3):369-375.[3].EdmondsonSD,etal.DiscoveryofVibegron:APotentandSelectiveβ3AdrenergicReceptorAgonistfortheTreatmentofOveractiveBladder.JMedChem.2016;59(2):609-623.[4].GotohD,etal.Effectsofanewβ3-adrenoceptoragonist,vibegron,onneurogenicbladderdysfunctionandremodelinginmicewithspinalcordinjury.NeurourolUrodyn.2020;39(8):2120-2127.[5].FurutaA,etal.Additiveeffectsofintravenousandintravesicalapplicationofvibegron,aβ3-adrenoceptorago