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Dalcotidine

Catalog No. T31195   CAS 120958-90-9
Synonyms: KU 1257, KU-1257

Dalcotidine (KU 1257) is a novel histamine H2 receptor antagonist with histamine H9 receptor antagonistic activity and antisecretory effects.The Ki value for binding to guinea pig cerebral cortex was 0.040 The KB value for antagonism of histamine-induced positive chronotropic responses in the right atrium of isolate guinea pigs was 0.041.Dalcotidine improves the quality of ulcer healing, and may contribute to a reduction in ulcer recurrence and relapse rates.

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Dalcotidine Chemical Structure
Dalcotidine, CAS 120958-90-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 143.00
5 mg In stock $ 360.00
10 mg In stock $ 530.00
25 mg In stock $ 859.00
50 mg In stock $ 1,180.00
100 mg In stock $ 1,590.00
500 mg In stock $ 3,190.00
1 mL * 10 mM (in DMSO) In stock $ 358.00
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Purity: 98.34%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Dalcotidine (KU 1257) is a novel histamine H2 receptor antagonist with histamine H9 receptor antagonistic activity and antisecretory effects.The Ki value for binding to guinea pig cerebral cortex was 0.040 The KB value for antagonism of histamine-induced positive chronotropic responses in the right atrium of isolate guinea pigs was 0.041.Dalcotidine improves the quality of ulcer healing, and may contribute to a reduction in ulcer recurrence and relapse rates.
Targets&IC50 H2 receptor:0.04 mumol/l
In vivo KU-1257 (10-50 mg/kg x 2/day; oral; rats)markedly promoted the well-balanced healing of gastric ulcers, as evidenced by the reduction of ulcers, regeneration of mucosa and proliferation of connective tissue. KU-1257 caused an increase in gastric mucus secretion in the regenerated mucosa around the gastric ulcers. KU-1257 is characterized by a potent promoting action on the healing of chronic ulcers, suggesting that the increase in gastric mucus secretion might be associated with the antiulcer actions of KU-1257 in part.[2]
Synonyms KU 1257, KU-1257
Molecular Weight 319.44
Formula C18H29N3O2
CAS No. 120958-90-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 3.6 mg/mL (11.27 mM)

TargetMolReferences and Literature

1. Sekiguchi H, et al. Pharmacological profiles of the new histamine H2-receptor antagonist N-ethyl-N'-[3-[3-(piperidinomethyl)phenoxy] propyl] urea. Arzneimittelforschung. 1993;43(2):129-133. 2. Sekiguchi H, et al. Healing-promoting action of the new histamine H2-receptor antagonist N-ethyl-N'-[3-[3-(piperidinomethyl)phenoxy]propyl]urea with dual action on chronic gastric and duodenal ulcers induced by acetic acid in rats. Arzneimittelforschung. 1993;43(2):139-143. 3. Sekiguchi H, et al. Effects of the new histamine H2-receptor antagonist N-ethyl-N'-[3-[3-(piperidinomethyl)phenoxy]propyl] urea with potent gastric mucosal protective activity on acute gastric lesions and duodenal ulcers in rats. Arzneimittelforschung. 1993;43(2):134-138. 4. Sekiguchi H, et al. Influence of KU-1257 on the recurrence and relapse of acetic acid-induced chronic gastric ulcers in rats. Nihon Yakurigaku Zasshi. 1996;107(2):67-78.

Related compound libraries

This product is contained In the following compound libraries:
GPCR Compound Library Membrane Protein-targeted Compound Library Bioactive Compound Library Neuronal Signaling Compound Library Bioactive Compounds Library Max

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Keywords

Dalcotidine 120958-90-9 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor KU 1257 KU-1257 KU1257 inhibitor inhibit

 

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