TY-11345
TY-11345 is an orally active gastric mucosal H+/K+-ATPase inhibitor, with IC50 values of 5.8 μM (Reference 1) and 3.3 μM (Reference 2) at pH 6.0, respectively. TY-11345 inhibits basal gastric acid secretion stimulated by Tetragastrin (HY-125556) and Pentagastrin (HY-A0261), and prevents gastric and duodenal injuries in rats. TY-11345 can be used in the research of peptic ulcer disease and acid-related gastrointestinal diseases.
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- No. CAS: 137927-14-1
- Fòrmula: C18H19N3NaO2S
- Peso molecular:364.42
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Actividad biológica
TY-11345 potently inhibits H+/K+-ATPase activity in purified rabbit gastric mucosal microsomes, with an IC50 of 5.8 μM at pH 6.0 and 9.9 μM at pH 7.4; furthermore, it achieves near-maximal inhibitory effect within 10 min of pre-incubation at pH 6.0[1].
TY-11345 potently inhibits H+/K+-ATPase isolated from rabbit gastric mucosa, with an IC50 value of 3.3 μM at pH 6.0 and 9.7 μM at pH 7.4[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
TY-11345 (0.1-100 mg/kg; intravenous, intradermal, oral administration; single dose) potently inhibits basal gastric acid secretion in pylorus-ligated rats via multiple routes, with an ED50 of 1.2 mg/kg following duodenal administration[1].
TY-11345 (0.3-3.0 mg/kg; p.o.; single administration) potently prevents water immersion stress-induced gastric injury in rats, with an ED50 of 0.92 mg/kg[1].
TY-11345 (0.3-3.0 mg/kg; p.o.; single administration) potently prevents Indomethacin (HY-14397)-induced gastric injury in rats, with an ED50 of 0.64 mg/kg[1].
TY-11345 (3-30 mg/kg; p.o.; single administration) potently prevents Ethanol-induced gastric injury in rats, with an ED50 of 10.5 mg/kg[1].
TY-11345 (0.3-3.0 mg/kg; p.o.; twice-daily dosing) potently prevents mepirizole (HY-103595)-induced duodenal ulcers in rats, with an ED50 of 0.90 mg/kg[1].
TY-11345 (3-30 mg/kg; p.o.; once daily; 14 days) potently promotes the healing of chronic gastric ulcers induced by Acetic acid (HY-Y0319) in rats, with an ED50 of 16.5 mg/kg/day[1].
TY-11345 (1 mg/kg; intravenous injection; single administration) achieves a maximum inhibition rate of 67.1% against pentagastrin-stimulated gastric acid secretion in rats, and maintains an inhibitory effect of 54.9% at 3 h post-administration[2].
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 with tetragastrin stimulation)[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.; single dose
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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 in the 30 to 60-minute period.
Achieved an ED50 value of 0.22 mg/kg in the 150 to 180-minute period.
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Animal Model:Sprague-Dawley (male, 232-267 g, pylorus-ligated model)[1]
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Dosage:0.1-1.0 mg/kg (i.v., immediate post-ligation); 1-10 mg/kg (i.d., immediate post-ligation); 3-30 mg/kg (p.o., 0.5 hours pre-ligation); 10-100 mg/kg (p.o., 19 hours pre-ligation)
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Administration:i.v.; single dose (immediately post-ligation); i.d.; single dose (immediately post-ligation); p.o.; single dose (0.5 hours pre-ligation); p.o.; single dose (19 hours pre-ligation)
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Result:Dose-dependently inhibited gastric acid secretion (volume, acid concentration, total acid output) across all administration routes.
Achieved an ED50 value of 1.2 mg/kg (i.d.).
Achieved an ED50 value of 4.0 mg/kg (p.o., 0.5 hours pre-ligation).
Achieved an ED50 value of 12.7 mg/kg (p.o., 19 hours pre-ligation).
Completely inhibited acid output at 10 mg/kg i.d.
Sustained antisecretory effect for more than 24 hours after oral administration.
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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 (30 minutes pre-stress)
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Result:Dose-dependently inhibited water-immersion stress-induced gastric lesions, with inhibitory percentages of 31%, 37%, and 84% at 0.3, 1.0, and 3.0 mg/kg, respectively.
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 (30 minutes pre-Indomethacin)
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Result:Dose-dependently inhibited Indomethacin-induced gastric lesions, with inhibitory percentages of 36%, 52%, and 87% at 0.3, 1.0, and 3.0 mg/kg, respectively.
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 (30 minutes pre-Ethanol)
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Result:Dose-dependently inhibited Ethanol-induced gastric lesions, with inhibitory percentages of 10%, 46%, and 88% at 3, 10, and 30 mg/kg, respectively.
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 (30 minutes pre-mepirizole and 9 hours post-Mepirizole)
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Result:Dose-dependently inhibited Mepirizole-induced duodenal ulcers, with inhibitory percentages of 8%, 64%, and 87% at 0.3, 1.0, and 3.0 mg/kg (total two doses), respectively.
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:Dose-dependently accelerated healing of Acetic acid-induced chronic gastric ulcers, with inhibitory percentages of the ulcer index of 52% and 82% at 10 and 30 mg/kg/day, respectively.
Achieved an ED50 value of 16.5 mg/kg/day.
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Animal Model:strain not specified[2]
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Dosage:1 mg/kg
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Administration:i.v.; single dose
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Result:Produced a maximum 67.1% inhibition of Pentagastrin-stimulated gastric acid secretion.
Maintained 54.9% inhibition 3 hours after dosing.
Chemical Information
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No. CAS 137927-14-1
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Peso molecular 364.42
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Fòrmula C18H19N3NaO2S
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SMILES
O=S(C1C2=NC=CC(OC)=C2CCCC1)C3=NC4=C(N3)C=CC=C4.[Na]
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Yamaguchi T, et al. Biochemical and pharmacological properties of a newly synthesized proton pump (H+/K(+)-ATPase) inhibitor, TY-11345 in experimental animals. Japanese journal of pharmacology. 1993 Aug;62(4):363-71. [Content Brief]
[2]. Yamada S, et al. Synthesis and antiulcer activities of novel 2-[(6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl)sulfinyl]-1H- benzimidazole analogues. Chemical & pharmaceutical bulletin. 1994 Mar;42(3):718-20. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TY-11345 Related Classifications
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