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Art. -Nr.: HY-116596

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Histamine H2 receptor antagonist-1

Antiulcer Agent 3 is a orally active histamine H₂-receptor competitive antagonist (pA₂ = 6.7). Antiulcer Agent 3 reduces gastric acid secretion. Antiulcer Agent 3 reduces gastric lesions in water-immersion stress-induced ulcer rat models. Antiulcer Agent 3 protects against HCl-ethanol-induced gastric lesions in rats. Antiulcer Agent 3 can be used for the research of peptic ulcer disease.

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CAS. Nr.: 127966-78-3
Formel: C₁₉H₃₀N₂O₃S
Molecular Weight:366.52

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Histamine H2 receptor antagonist-1 Chemical Structure

CAS. Nr.: 127966-78-3

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
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Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

H₂ Receptor

6.7 (pA2)

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

Antiulcer Agent 3 (compound 8) acts as a competitive histamine H₂ receptor antagonist in isolated guinea pig right atria, with a pA₂ value of 6.7^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Antiulcer Agent 3 (Compound 8) (30 mg/kg; intradermal injection; single administration) inhibits gastric acid secretion in conscious rats with gastric fistula. At the dose of 30 mg/kg, its inhibition rate reaches 79.5%, with an ED₅₀ of 12.9 mg/kg^[1].
Antiulcer Agent 3 (administered orally; single dose; 5 minutes before stress) inhibits water-immersion stress-induced gastric ulcers in rats, with an oral ED₅₀ of 13.3 mg/kg^[1].
Antiulcer Agent 3 (oral administration; single dose) exhibits cytoprotective activity against hydrochloric acid-ethanol-induced gastric ulcers in rats, with an oral ED₅₀ of 43.7 mg/kg^[1].
Antiulcer Agent 3 (0.25-1.0 mg/kg; intravenous injection; single administration) inhibits Histamine (HY-B1204)-induced gastric acid secretion in conscious dogs with Heidenhain pouches, and exhibits significant long-acting activity at the dose of 1.0 mg/kg, with an ED₅₀ of 0.38 mg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Sprague-Dawley (male, 180-200 g, gastric fistula model)^[1]
Dosage:

30 mg/kg
Administration:

i.d.; single dose
Result:

Inhibited basal gastric acid secretion by 79.5%.
Achieved an ED₅₀ of 12.9 mg/kg for gastric acid antisecretory activity.

Animal Model:

LR beagle (male, 9-10 kg, Heidenhain pouch model)^[1]
Dosage:

0.25 mg/kg; 0.5 mg/kg; 1.0 mg/kg
Administration:

i.v.; single dose
Result:

Inhibited histamine-stimulated gastric acid secretion.
Produced a significant, long-lasting reduction in acid output at 1.0 mg/kg, with values significantly different from controls at p < 0.05 or p < 0.01 for multiple time points up to 180 minutes.

Chemical Information

CAS. Nr. 127966-78-3
Molecular Weight 366.52
Formel C₁₉H₃₀N₂O₃S
SMILES

O=C(NCCCOC1=CC=CC(CN2CCCCC2)=C1)CSCCO
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Ueda I, et al. Synthesis and pharmacological properties of N-[3-(3-(1-Piperidinylmethyl)phenoxy)propyl]-2-(2-hydroxyethylthio)- acetamide and related compounds as antiulcer agents. I. Chemical & pharmaceutical bulletin. 1990 Nov;38(11):3035-41. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Keywords

Histamine H2 receptor antagonist-1

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Biologische Aktivität
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- In Vivo
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Histamine H2 receptor antagonist-1

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

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Verweise

Calculators

Help & FAQs

Histamine H2 receptor antagonist-1 Related Classifications

HY-116596 Related Classifications

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