IndomethacinIndomethacin
MedChemExpress (MCE)
HY-14397
53-86-1
Indometacin
99.91%
4°C, protect from light *In solvent : -80°C, 1 year
-20°C, 6 months (protect from light)
Room temperature in continental US
may vary elsewhere.
Indomethacin (Indometacin) is a potent, orally active COX1/2 inhibitor with IC50 values of 18 nM and 26 nM for COX-1 and COX-2, respectively. Indomethacin has anticancer activity and anti-infective activity. Indomethacin can be used for cancer, inflammation and viral infection research.
Indomethacin (Indometacin) (0-150 μM
24 hours
3LL-D122 cells) has anticancer activity in vitro[2].Indomethacin (Indometacin) (0-1000 μM) protects the host cells from damage caused by the virus through activates PKR, resulting in elF2α phosphorylation, and in turn shutting of translation of viral protein and inhibiting replication of the virus (IC50=2μM)[3].
Indomethacin can be used to induce gastric ulcer models. After oral administration, the drug is absorbed rapidly and completely, although there are interindividual and intraindividual variations. Typically, the plasma peak concentration (2-3 μg/mL) is 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]. .f12{ font-size: 12px
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} 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 Mmodeling 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)
Human COX-1 18 nM (IC50, in CHO cells) Human COX-2 26 nM (IC50, in CHO cells)
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[1]. Riendeau D, et, al. Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX-2 inhibitor. Br J Pharmacol. 1997 May
121(1):105-17. [Content Brief]
[2]. Eli Y, et, al. Comparative effects of indomethacin on cell proliferation and cell cycle progression in tumor cells grown in vitro and in vivo. Biochem Pharmacol. 2001 Mar 1
61(5):565-71. [Content Brief]
[3]. Amici C, et, al. Inhibition of viral protein translation by indomethacin in vesicular stomatitis virus infection: role of eIF2α kinase PKR. Cell Microbiol. 2015 Sep
17(9):1391-404. [Content Brief]
[4]. Helleberg L, et, al. Clinical Pharmacokinetics of indomethacin. Clin Pharmacokinet. 1981 Jul-Aug
6(4):245-58. [Content Brief]
[5]. Sabiu S, et, al. Indomethacin-induced gastric ulceration in rats: Protective roles of Spondias mombin a nd Ficus exasperate. Toxicol Rep. 2015 Jan 8:2:261-267. [Content Brief]
[6]. Danisman B, et, al, Carnosic Acid Ameliorates Indomethacin-Induced Gastric Ulceration in Rats by Alleviating Oxidative Stress and Inflammation. Biomedicines. 2023 Mar 9
11(3):829. [Content Brief]
