KW-5805
KW-5805 is an orally effective anti-ulcer agent that potently inhibits gastric injury induced by various necrotizing agents. KW-5805 enhances the activity of gastric mucosal glucosamine synthetase, increases the levels of gastric adherent mucus and mucosal glycoproteins, and promotes the biosynthesis, storage and secretion of gastric mucus. KW-5805 inhibits the reduction of gastric mucosal blood volume and oxygen supply caused by hemorrhagic shock. KW-5805 suppresses the development of experimental gastric and duodenal ulcers, necrotizing agent-induced gastric mucosal injury, and induced gastric acid secretion. KW-5805 can be used in ulcer-related research.
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- CAS No.: 113302-01-5
- Formule: C19H28Cl3N3O
- Masse moléculaire:420.80
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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
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
KW-5805 (10-30 mg/kg; p.o.) significantly maintains gastric mucosal blood volume and oxygen supply adequacy during hemorrhagic shock, while the 30 mg/kg oral dose significantly alleviates ischemia-reperfusion-induced gastric mucosal vascular injury in male Donryu rats[1].
KW-5805 (p.o.) potently inhibits water immersion stress-induced gastric ulcers in male Donryu rats with an ED50 of 3.5 mg/kg; potently inhibits aspirin-induced gastric ulcers with an ED50 of 1.2 mg/kg; potently inhibits indomethacin-induced gastric ulcers with an ED50 of 10.0 mg/kg; potently inhibits mepirizole-induced duodenal ulcers with an ED50 of 6.8 mg/kg; potently inhibits 0.6 N HCl-induced gastric mucosal lesions with an oral ED50 of 39.8 mg/kg; and potently inhibits acidified taurocholate-induced gastric mucosal lesions with an oral ED50 of 11.8 mg/kg[2].
KW-5805 (4.5-10 mg/kg; p.o., s.c.) potently inhibits gastric mucosal injury induced by 99.5% ethanol in male Donryu rats, with an oral ED50 of 4.5 mg/kg, and oral or subcutaneous administration at a dose of 10 mg/kg significantly alleviates the injury[2].
KW-5805 (3-30 mg/kg; intradermal injection) slightly inhibits gastric acid secretion in pylorus-ligated male Donryu rats, and at the dose of 30 mg/kg i.d., it significantly reduces gastric juice volume and acid output by 30%[2].
KW-5805 (10-30 mg/kg; intravenous administration) significantly inhibits acetylcholine- and tetragastrin-stimulated gastric acid secretion in male Donryu rats with acute gastric fistula2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Donryu (male, 190-210 g)[1]
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Dosage:30 mg/kg
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Administration:p.o.
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Result:Raised gastric adherent mucus volume relative to saline.
Elevated mucosal glycoprotein hexose content versus saline.
Boosted gastric mucosal glucosamine synthetase activity compared with saline.
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Animal Model:Donryu (male, 190-210 g, hemorrhagic shock-induced gastric mucosal injury model)[1]
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Dosage:10-30 mg/kg
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Administration:p.o.; 1 hour before induction of hemorrhagic shock
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Result:Attenuated hemorrhagic shock-induced reductions in gastric mucosal blood volume and oxygen availability at all time points.
Inhibited ischemia-reperfusion-mediated Evans blue extravasation in gastric mucosa at 30 mg/kg.
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Animal Model:Donryu rats (male, 190-210 g, 99.5% ethanol-induced gastric mucosal lesions model, 36-hour fasted)[2]
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Dosage:10 mg/kg (p.o.); 10 mg/kg (s.c.)
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Administration:p.o.; single dose (30 minutes before ethanol); s.c.; single dose (30 minutes before ethanol)
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Result:Lowered lesion index to 12 mm (10 mg/kg p.o.) and 10 mm (10 mg/kg s.c.).
Possessed superior cytoprotective potency versus pirenzepine and cimetidine.
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Animal Model:Donryu rats (male, 190-210 g, pylorus-ligated gastric hypersecretion model, 48-hour fasted)[2]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:i.d.; single dose (immediate post-ligation)
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Result:Cut gastric volume to 2.8 mL with 30% suppression at 30 mg/kg i.d.
Lowered total acid output to 82.0 μEq/hr with 30% suppression at 30 mg/kg i.d.
Displayed weaker antisecretory activity, 3-10-fold less potent than pirenzepine and cimetidine.
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Animal Model:Donryu rats (male, 190-210 g, acute gastric fistula gastric hypersecretion model, 24-hour fasted)[2]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:i.v.; single dose (30 minutes before secretagogue)
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Result:Suppressed methacholine-stimulated gastric acid secretion at 10 and 30 mg/kg i.v.
Exhibited equivalent inhibition to 1 mg/kg i.p. pirenzepine against methacholine-induced acid output at 30 mg/kg i.v.
Inhibited tetragastrin-evoked gastric acid secretion at 30 mg/kg i.v.
Chemical Information
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CAS No. 113302-01-5
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Masse moléculaire 420.80
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Formule C19H28Cl3N3O
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SMILES
CCN(CC)CCNC1C2=CC=CC=C2OCC3=NC=CC=C31.[H]Cl.[H]Cl.[H]Cl
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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
[1]. Tanaka H, Kosaka N, Tomaru A, et al.. Augmentation of the gastric mucosal defense mechanism induced by KW-5805, a novel antiulcer agent. Scandinavian journal of gastroenterology. Supplement. 1989;162:170-3. [Content Brief]
[2]. Kosaka N, Tanaka H, Tomaru A, et al.. Effects of KW-5805, a new antiulcer agent, on experimental gastric and duodenal ulcers, gastric mucosal lesions by necrotizing agents and gastric acid secretion. Japanese journal of pharmacology. 1994 Aug;65(4):305-12. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KW-5805 Related Classifications
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