Vonoprazan-TAK-438-free-base-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEVonoprazanCat.No.:HY-100007CASNo.:881681-00-1Synonyms:TAK-438freebase分?式:C??H??FN?O?S分?量:345.39作?靶點:ProtonPump;Bacterial作?通路:MembraneTransporter/IonChannel;Anti-infection儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(289.53mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.8953mL14.4764mL28.9528mL5mM0.5791mL2.8953mL5.7906mL10mM0.2895mL1.4476mL2.8953mL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，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?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：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(7.24mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.24mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.24mM);ClearsolutionBIOLOGICALACTIVITY?物活性Vonoprazan(TAK-438freebase)?種質(zhì)?泵抑制劑(PPI)，?效的，具有?服活性的鉀競爭性酸阻斷劑(potassium-competitiveacidblocker,P-CAB)，具有抗分泌活性。在pH為6.5時，Vonoprazan抑制豬胃微粒體中的H+,K+-ATPase酶活性，IC50值為19nM。Vonoprazan被開發(fā)?于研究胃酸相關(guān)疾病，如胃?管反流病和消化性潰瘍。Vonoprazan可?于根除幽門螺桿[1][2][3]。IC50&TargetIC50:19nM(porcinegastricH+,K+-ATPase,atpH6.5)[2]體外研究Vonoprazan(0.1nM-10μM;30minutes)exhibitsporcinegastricH+,K+-ATPaseactivityinaconcentration-dependentmanner[2].VonoprazandoesnotinhibitNa+,K+-ATPaseactivity,evenatconcentrations500timeshigherthantheirIC50valuesagainstgastricH+,K+-ATPaseactivity[2].體內(nèi)研究Vonoprazan(1-4mg/kg;p.o.)completelyinhibitsbasaland2-deoxy-D-glucose(200mg/kg;s.c.)-stimulatedgastricacidsecretionatthe4mg/kgdoseinrats[2].AnimalModel:Male7-or8-week-oldSprague-Dawleyrat[2]Dosage:0.5mg/kg,1mg/kg,2mg/kg,4mg/kgAdministration:OraladministrationResult:Inhibitedbasalgastricacidsecretioninadose-dependentmanner.戶使?本產(chǎn)品發(fā)表的科研?獻?BrJClinPharmacol.2019Jul;85(7):1454-1463.?DrugMetabDispos.2016Oct;44(10):1543-9.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].SugimotoM,etal.RoleofVonoprazaninHelicobacterpyloriEradicationTherapyinJapan.FrontPharmacol.2019Jan15;9:1560.[2].ArikawaY,etal.Discoveryofanovelpyrrolederivative1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanaminefumarate(TAK-438)asapotassium-competitiveacidblocker(P-CAB).JMedChem,2012,55(9),4446-4456.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[3].HoriY,etal.1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanaminemonofumarate(TAK-438),anovelandpotentpotassium-competitiveacidblockerforthetreatmentofacid-relateddiseases.JPharmacolExpTher,2010,335(1),McePdfHeightCaution:Producthasnotbeenfullyvalidat