Nepaprazole sodium
Nepaprazole sodium (rel-TY-11345) is a proton pump H+/K+-ATPase inhibitor. Nepaprazole sodium inhibits H+/K+-ATPase activity in rabbit gastric mucosal microsomes, with IC50 values of 5.8 μM and 9.9 μM at pH 6.0 and pH 7.4, respectively, and its inhibitory activity is enhanced under weakly acidic conditions. Nepaprazole sodium inhibits basal and Tetragastrin (HY-125556)-stimulated gastric acid secretion. Nepaprazole sodium can be used in studies on gastric proton pump function, gastric acid secretion, and mechanisms related to peptic ulcers.
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- CAS No.: 157564-11-9
- Formule: C18H19N3NaO2S
- Masse moléculaire:364.42
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
IC50 & Target
[1]|
H+/K+-ATPase 5.8 μM (IC50, pH 6.0) |
H+/K+-ATPase 9.9 μM (IC50, pH 7.4) |
In Vitro
Pretreatment with nepaprazole sodium (rel-TY-11345) for 30 min inhibits the activity of rabbit gastric mucosal microsomal H+/K+-ATPase in a concentration-dependent manner, with IC50 values of 5.8 μM and 9.9 μM at pH 6.0 and pH 7.4, respectively[1].
Nepaprazole sodium (10 μM; pH 6.0) inhibits rabbit gastric mucosal microsomal H+/K+-ATPase in a time-dependent manner, reaches near-maximal effect at approximately 10 min, and shows an inhibition rate of about 85% after 30 min of pre-incubation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Nepaprazole sodium (3, 10, 30 mg/kg; p.o.; 0.5 h before pyloric ligation) dose-dependently inhibits basal gastric acid secretion in pylorus-ligated rats, with an ED50 of 4.0 mg/kg[1].
Nepaprazole sodium (1, 3, 10 mg/kg; intraduodenal administration) dose-dependently inhibits basal gastric acid secretion in pylorus-ligated rats, almost completely suppressing acid output at 10 mg/kg, with an ED50 of 1.2 mg/kg[1].
Nepaprazole sodium (10, 30, 100 mg/kg; p.o.; 19 h before pyloric ligation) significantly reduces gastric acid output in pylorus-ligated rats even at approximately 24 h post-administration, with an ED50 of 12.7 mg/kg[1].
Nepaprazole sodium (0.3, 1, 3 mg/kg; p.o.; 30 min prior to stress) dose-dependently inhibits water-immersion restraint stress-induced gastric mucosal injury in male Sprague-Dawley rats, with an ED50 of 0.92 mg/kg[1].
Nepaprazole sodium (0.3, 1, 3 mg/kg; p.o.; 30 min prior to indomethacin) dose-dependently inhibits indomethacin (HY-14397)-induced gastric mucosal injury in male Sprague-Dawley rats, with an ED50 of 0.64 mg/kg[1].
Nepaprazole sodium (3, 10, 30 mg/kg; p.o.; 30 min prior to ethanol) dose-dependently inhibits absolute ethanol-induced gastric mucosal injury in male Sprague-Dawley rats, with an ED50 of 10.5 mg/kg[1].
Nepaprazole sodium (0.3, 1, 3 mg/kg; p.o.; administered twice) dose-dependently inhibits Mepirizole (HY-103595)-induced duodenal ulcers in male Sprague-Dawley rats, with an ED50 of 0.90 mg/kg[1].
Nepaprazole sodium (3, 10, 30 mg/kg/day; p.o.; once daily; for 14 consecutive days) promotes ulcer healing in acetic acid-induced chronic gastric ulcer models of male Sprague-Dawley rats. At doses of 10 and 30 mg/kg, the ulcer index decreases by 52% and 82%, respectively, with an ED50 of 16.5 mg/kg/day[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 213-364 g, Ghosh & Schild model)[1]
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Dosage:0.3 mg/kg; 0.5 mg/kg; 1.0 mg/kg
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Administration:i.v.
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Result:Potently suppressed tetragastrin-stimulated gastric acid secretion for at least 180 minutes.
Achieved an ED50 value of 0.39 mg/kg during the 30-60 minute period.
Achieved an ED50 value of 0.22 mg/kg during the 150-180 minute period.
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Animal Model:Sprague-Dawley (male, 190-273 g, water-immersion stress-induced model)[1]
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Dosage:0.3 mg/kg; 1.0 mg/kg; 3.0 mg/kg
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Administration:p.o.; single dose
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Result:Reduced lesion index by 31%, 37%, and 84% respectively, relative to vehicle controls.
Achieved an ED50 value of 0.92 mg/kg.
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Animal Model:Sprague-Dawley (male, 178-285 g, indomethacin-induced model)[1]
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Dosage:0.3 mg/kg; 1.0 mg/kg; 3.0 mg/kg
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Administration:p.o.; single dose
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Result:Reduced lesion index by 36%, 52%, and 87% respectively, relative to vehicle controls.
Achieved an ED50 value of 0.64 mg/kg.
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Animal Model:Sprague-Dawley (male, 215-315 g, ethanol-induced model)[1]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:p.o.; single dose
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Result:Reduced lesion index by 10%, 46%, and 88% respectively, relative to vehicle controls.
Achieved an ED50 value of 10.5 mg/kg.
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Animal Model:Sprague-Dawley (male, 215-285 g, mepirizole-induced model)[1]
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Dosage:0.3 mg/kg; 1.0 mg/kg; 3.0 mg/kg
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Administration:p.o.; two doses
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Result:Reduced ulcer index by 8%, 64%, and 87% respectively, relative to vehicle controls.
Achieved an ED50 value of 0.90 mg/kg.
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Animal Model:Sprague-Dawley (male, 192-218 g, acetic acid-induced chronic model)[1]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:p.o.; daily; 14 days
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Result:Reduced ulcer index by 52% and 82% respectively at the 10 mg/kg and 30 mg/kg doses, relative to vehicle controls.
Achieved an ED50 value of 16.5 mg/kg/day.
Chemical Information
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CAS No. 157564-11-9
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Masse moléculaire 364.42
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Formule C18H19N3NaO2S
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SMILES
S(=O)([C@]1(C=2C(=C(OC)C=CN2)CCCC1)[H])C=3NC=4C(N3)=CC=CC4.[Na]
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Synonyms
rel-TY-11345
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Nepaprazole sodium Related Classifications
HY-19153A Related Classifications
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