Medchemexpress/TAK-438(Synonyms: Vonoprazan Fumarate)/HY-15295/10mM*1mL in DMSO-免疫在线蚂蚁淘旗下平台

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商品详细Medchemexpress/TAK-438(Synonyms: Vonoprazan Fumarate)/HY-15295/10mM*1mL in DMSO

Medchemexpress/TAK-438(Synonyms: Vonoprazan Fumarate)/HY-15295/10mM*1mL in DMSO

商品编号： HY-15295-10mM*1mLinDMSO

品牌： MedChemExp

市场价： ¥5940.00

美元价： 3564.00

产地：美国(厂家直采)

公司：

产品分类：小分子

公司分类： Small_molecule

联系Q Q： 3392242852

电话号码： 4000-520-616

电子邮箱： info@ebiomall.com

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商品介绍

TAK-438isanovelP-CAB(potassium-competitiveacidblocker)thatreversIBLyinhibitsH+/K+,ATPasewithIC50of19nM(pH6.5),controlsgastricacidsecretion.

Description	TAK-438isanovelP-CAB(potassium-competitiveacidblocker)thatreversiblyinhibitsH+/K+,ATPasewithIC50of19nM(pH6.5),controlsgastricacidsecretion.IC50value:19nM[1]Target:H+/K+ATPaseinvitro:TAK-438isapyrrolederivativewithachemicalstructurethatiscompletelydifferentfromtheP-CABsdevelopedtodate.TAK-438inhibitsgastricH+,K+-ATPaseactivityinaconcentration-dependentmanner.Underneutralconditions(pH7.5),theinhibitoryactivityofTAK-438isalmostthesameasthatunderweaklyacidicconditions(pH6.5).TAK-438doesnotinhibitNa+,K+-ATPaseactivityevenatconcentration500timeshigherthantheirIC50valuesagainstgastricH+,K+-ATPaseactivity.TAK-438inhibitsgastricH+,K+-ATPaseinaK+-competitivemannerwithKiof3nM[2].invivo:TAK-438inhibitsbasalgastricacidsecretioninadose-dependentmanner,andtheID50valueis1.26mg/kg.IntravenousadmiNISTrationofTAK-438dose-dependentlyincreasesthepHofthegastricperfusate,andtheincreaseinpHissustainedfor5hafteradministration.Atthe1mg/kgdose,thepHplateaues90minafteradministration,andthehighestpHvaluereachedis5.9[2].Inaddition,TAK-438showsapotentandlonger-lastinginhibitoryeffectonthehistamine-stimulatedgastricacidsecretioninratsanddogs.TAK-438showssignificantantisecretoryactivitythroughhighaccumulationandslowclearancefromthegastrictissue.TAK-438isunaffectedbythegastricsecretorystate,unlikePPIs[3].
References	[1].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].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),231-238. [3].HoriY,etal.AstudycomparingtheantisecretoryeffectofTAK-438,anovelpotassium-competitiveacidblocker,withlansoprazoleinanimals.JPharmacolExpTher,2011,337(3),797-804.

Description

TAK-438isanovelP-CAB(potassium-competitiveacidblocker)thatreversiblyinhibitsH+/K+,ATPasewithIC50of19nM(pH6.5),controlsgastricacidsecretion.IC50value:19nM[1]Target:H+/K+ATPaseinvitro:TAK-438isapyrrolederivativewithachemicalstructurethatiscompletelydifferentfromtheP-CABsdevelopedtodate.TAK-438inhibitsgastricH+,K+-ATPaseactivityinaconcentration-dependentmanner.Underneutralconditions(pH7.5),theinhibitoryactivityofTAK-438isalmostthesameasthatunderweaklyacidicconditions(pH6.5).TAK-438doesnotinhibitNa+,K+-ATPaseactivityevenatconcentration500timeshigherthantheirIC50valuesagainstgastricH+,K+-ATPaseactivity.TAK-438inhibitsgastricH+,K+-ATPaseinaK+-competitivemannerwithKiof3nM[2].invivo:TAK-438inhibitsbasalgastricacidsecretioninadose-dependentmanner,andtheID50valueis1.26mg/kg.IntravenousadmiNISTrationofTAK-438dose-dependentlyincreasesthepHofthegastricperfusate,andtheincreaseinpHissustainedfor5hafteradministration.Atthe1mg/kgdose,thepHplateaues90minafteradministration,andthehighestpHvaluereachedis5.9[2].Inaddition,TAK-438showsapotentandlonger-lastinginhibitoryeffectonthehistamine-stimulatedgastricacidsecretioninratsanddogs.TAK-438showssignificantantisecretoryactivitythroughhighaccumulationandslowclearancefromthegastrictissue.TAK-438isunaffectedbythegastricsecretorystate,unlikePPIs[3].

References

[1].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].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),231-238.
[3].HoriY,etal.AstudycomparingtheantisecretoryeffectofTAK-438,anovelpotassium-competitiveacidblocker,withlansoprazoleinanimals.JPharmacolExpTher,2011,337(3),797-804.

PreparingStockSolutions

ConcentrationVolumeMass	1mg	5mg	10mg

1mM	2.1670mL	10.8352mL	21.6704mL
5mM	0.4334mL	2.1670mL	4.3341mL
10mM	0.2167mL	1.0835mL	2.1670mL

Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.

References

[1].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].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),231-238.
[3].HoriY,etal.AstudycomparingtheantisecretoryeffectofTAK-438,anovelpotassium-competitiveacidblocker,withlansoprazoleinanimals.JPharmacolExpTher,2011,337(3),797-804.

MolecularWeight

461.46

Formula

C₂₁H₂₀FN₃O₆S

CASNo.

1260141-27-2

Storage

Powder	-20°C	3years
	4°C	2years
Insolvent	-80°C	6months
	-20°C	1month

Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

10mMinDMSO

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:99.97%

SelectBatch: