Cart
sales@molnova.com
TAK-438 free base
CAS No. 881681-00-1
TAK-438 free base( Vonoprazan | TAK438 free base )
Catalog No. M16393 CAS No. 881681-00-1
A novel potent, oral potassium-competitive acid blocker (P-CAB) that potently inhibits H+,K+-ATPase with IC50 of 19 nM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 50MG | 26 | Get Quote |
|
| 100MG | Get Quote | Get Quote |
|
| 200MG | Get Quote | Get Quote |
|
| 500MG | Get Quote | Get Quote |
|
| 1G | Get Quote | Get Quote |
|
Biological Information
-
Product NameTAK-438 free base
-
NoteResearch use only, not for human use.
-
Brief DescriptionA novel potent, oral potassium-competitive acid blocker (P-CAB) that potently inhibits H+,K+-ATPase with IC50 of 19 nM.
-
DescriptionA novel potent, oral potassium-competitive acid blocker (P-CAB) that potently inhibits H+,K+-ATPase with IC50 of 19 nM; completely inhibits basal and 2-deoxy-d-glucose-stimulated gastric acid secretion in rats (4mg/kg, p.o.); increases the pH of gastric perfusate to a higher value, and sustains longer than those of lansoprazole or SCH28080; a clinical candidate for the treatment of gastroesophageal reflux disease (GERD), peptic ulcer, and other acid-related diseases.Ulcer Phase 3 Clinical(In Vitro):Vonoprazan (0.1 nM-10 μM; 30 minutes) exhibits porcine gastric H+, K+-ATPase activity in a concentration-dependent manner.Vonoprazan does not inhibit Na+,K+-ATPase activity, even at concentrations 500 times higher than their IC50 values against gastric H+,K+-ATPase activity.(In Vivo):Vonoprazan (1-4 mg/kg; p.o.) completely inhibits basal and 2-deoxy-D-glucose (200 mg/kg; s.c.)-stimulated gastric acid secretion at the 4 mg/kg dose in rats.
-
In VitroVonoprazan (0.1 nM-10 μM; 30 minutes) exhibits porcine gastric H+, K+-ATPase activity in a concentration-dependent manner.Vonoprazan does not inhibit Na+,K+-ATPase activity, even at concentrations 500 times higher than their IC50 values against gastric H+,K+-ATPase activity.
-
In VivoVonoprazan (1-4 mg/kg; p.o.) completely inhibits basal and 2-deoxy-D-glucose (200 mg/kg; s.c.)-stimulated gastric acid secretion at the 4 mg/kg dose in rats. Animal Model:Male 7- or 8-week-old Sprague-Dawley rat Dosage:0.5 mg/kg, 1 mg/kg, 2 mg/kg, 4 mg/kg Administration:Oral administration Result:Inhibited basal gastric acid secretion in a dose-dependent manner.
-
SynonymsVonoprazan | TAK438 free base
-
PathwayMembrane Transporter/Ion Channel
-
TargetProton Pump
-
RecptorProton Pump
-
Research AreaOther Indications
-
IndicationUlcer
Chemical Information
-
CAS Number881681-00-1
-
Formula Weight345.3912
-
Molecular FormulaC17H16FN3O2S
-
Purity>98% (HPLC)
-
SolubilityDMSO: ≥ 33 mg/mL
-
SMILESCNCC1=CN(C(=C1)C2=CC=CC=C2F)S(=O)(=O)C3=CN=CC=C3
-
Chemical Name1H-Pyrrole-3-methanamine, 5-(2-fluorophenyl)-N-methyl-1-(3-pyridinylsulfonyl)-
Shipping & Storage Information
-
Storage(-20℃)
-
ShippingWith Ice Pack
-
Stability≥ 2 years
Reference
1. Arikawa Y, et al. J Med Chem. 2012 May 10;55(9):4446-56.
2. Hori Y, et al. J Pharmacol Exp Ther. 2010 Oct;335(1):231-8.
3. Shin JM, et al. J Pharmacol Exp Ther. 2011 Nov;339(2):412-20.
molnova catalog
related products
-
Abeprazan hydrochlor...
Abeprazan hydrochloride (Fexuprazan hydrochloride) is an effective reversible potassium-competitive acid blocker with oral activity, inhibiting H+, K+ -atPase by competitive binding to potassium ions without acid activation.
-
(R)-Tegoprazan
(R)-Tegoprazan (example 3), a benzimidazole derivative, is a potent kidney H+/K+-ATPase inhibitor with an IC50 of 98 nM of canine kidney Na+/K+-ATPase.
-
Pantoprazole
A proton pump inhibitor that inhibits gastric acid secretion; works on gastric parietal cells to irreversibly inhibit (H+/K+)-ATPase function and suppress the production of gastric acid.
