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74252-25-8

74252-25-8 Structure

74252-25-8 Structure
IdentificationBack Directory
[Name]

INDOMETHACIN SODIUM SALT TRIHYDRATE
[CAS]

74252-25-8
[Synonyms]

Indometacin Sodium
INDOMETACIN FARNESIL
Sodium salt trihydrate
Indomethacin sodium hydrate
Indomethacin sodium trihydrate
Indomethacin sodium salt 3-hydrate
INDOMETHACIN SODIUM SALT TRIHYDRATE
sodium,2-[1-(4-chlorobenzoyl)-5-methoxy-2-methylindol-3-yl]acetate,trihydrate
1H-Indole-3-acetic acid, 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-, sodi um salt, trihydrate
1H-Indole-3-aceticacid, 1-(4-chlorobenzoyl)-5-Methoxy-2-Methyl-, sodiuM salt, hydrate (1:1:3)
[Molecular Formula]

C34H40ClNO4
[MOL File]

74252-25-8.mol
[Molecular Weight]

562.146
Chemical PropertiesBack Directory
[storage temp. ]

4°C, protect from light, stored under nitrogen
[solubility ]

DMSO: 5 mg/mL (11.53 mM)
[form ]

Solid
[color ]

Light yellow to yellow
[Water Solubility ]

Water: 33.33 mg/mL (76.83 mM)
Hazard InformationBack Directory
[Uses]

Anti-inflammatory.
[Brand name]

Indocin (Ovation).
[Hazard]

A poison by ingestion.
[in vivo]

Indomethacin sodium hydrate can be used to create gastric ulcer models. After oral administration, the drug is absorbed rapidly and completely, although there are interindividual and intraindividual variations. The plasma peak concentration of 2-3 μg/mL is typically reached within 1-2 hours. However, coadministration with food reduces and delays the peak concentration without affecting the total absorption. At therapeutic concentrations, 90% of Indomethacin is bound to albumin in the plasma[4].

Induction of gastric ulceration[5][6]
Background
Indomethacin can cause gastric ulceration by various mechanisms, including injury through inhibition of prostaglandin (PG) synthesis, reduction in local blood flow, regional irritation, and inhibition of tissue regeneration.
Specific Modeling Methods
Rat: albino Sprague-Dawley ? male ? adult (period: 2 weeks)
Administration: 100 mg/kg ? p.o. ? single dose
Note
(1) All animals fasted 24 h before drug administration.
(2) Indomethacin were dissolved in saline with 5% NaOH.
Modeling Indicators
Gastric tissue macroscopic alterations: Showed prominent mucosal folds and severe erosion, pronounced ulceration and bleeding foci in the gastric mucosa.
Histopathological changes: Showed severe erosion of the mucosa, reaching down to the lamina muscularis; observed hemorrhagic infiltration, edema in the submucosa, and severe hyperemia of the vessels.
Molecular changes: Showed intense Tnf-α expression.
Biochemical changes: Increased MDA, TOS levels, reduced TAS levels, CAT and GPx activities and GSH levels.
Correlated Product(s): Indomethacin sodium hydrate (HY-14397A)
Opposite Product(s): Carnosic acid (HY-N0644)

Animal Model:Male Sprague-Dawley rats[1]
Dosage:0.01-10 mg/kg
Administration:Oral administration; for 3 hours
Result:Inhibited the carrageenan-induced rat paw oedema (ED50=2.0?mg/kg) and hyperalgesia (ED50=1.5?mg/kg) in a dose-dependent manner.
Animal Model:Male C57BL/6J mice[2]
Dosage:10 mg/mL
Administration:Oral administration; daily, for 29 days
Result:Delayed the onset of tumor growth and the initial growth rate of the footpad tumors.
Safety DataBack Directory
[Symbol(GHS) ]


GHS08,GHS06
[Signal word ]

Danger
[Hazard statements ]

H300-H370
[Precautionary statements ]

P264-P270-P301+P310-P321-P330-P405-P501-P260-P264-P270-P307+P311-P321-P405-P501
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