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INDOMETHACIN SODIUM SALT TRIHYDRATE

Product NameINDOMETHACIN SODIUM SALT TRIHYDRATE
CAS74252-25-8
MFC34H40ClNO4
MW562.146
EINECS
MOL File74252-25-8.mol

Chemical Properties

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)
InChIKey	CFIGYZZVJNJVDQ-LMJOQDENSA-N
SMILES	C12C=CC(OC)=CC=1C(=C(C)N2C(=O)C1C=CC(Cl)=CC=1)CC(=O)OC/C=C(\C)/CC/C=C(\C)/CC/C=C(\C)/C

Usage And Synthesis

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=2.0mg/kg) and hyperalgesia (ED₅₀=1.5mg/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.

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