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.
For research use only. We do not sell to patients.
- CAS No.: 137927-14-1
- Formula: C18H19N3NaO2S
- Molecular Weight:364.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
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. Further protocols information, click here.
In Vivo
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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CAS No. 137927-14-1
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Molecular Weight 364.42
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
[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
HY-105015 Related Classifications
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