indomethacin

Indomethacin (Indomethacin) is a COX1 and COX2 inhibitor (IC50=18 26 nM) with blood-brain barrier permeability and non-selectivity. Indomethacin is a non-steroidal anti-inflammatory agent with anti-tumor and anti-infective activity.

Indomethacin farnesil (Infree) is a prodrug of indomethacin. It acts as a nonsteroidal anti-inflammatory drug (NSAID) and disease-modifying anti-rheumatic drug (DMARD).

Indomethacin heptyl ester is a non-selective inhibitor of both COX-1 and COX-2

Indomethacin-D4 is a deuterium labeled Indomethacin. Indomethacin is a potent and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells.

O-Desmethyl-N-deschlorobenzoyl indomethacin is a metabolite of the non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor indomethacin, formed from indomethacin in isolated rabbit hepatocytes. O-Desmethyl-N-deschlorobenzoyl indomethacin (600 μM) decreases the viability of HL-60 leukemia cells when cultured with glucose oxidase. It has also been used in the synthesis of prostaglandin D2 receptor antagonists.

Indomethacin sodium, a powerful and orally active inhibitor of COX1/2, exhibits IC50 values of 18 nM and 26 nM for COX-1 and COX-2, respectively. Apart from its potent anti-inflammatory effects, this compound possesses notable anticancer and anti-infective activities. Since it has such versatile attributes, it finds useful applicability in cancer, inflammation, and viral infection research [1] [2] [3].

Indomethacin sodium hydrate (Indometacin sodium hydrate) is an orally active, competitive and reversible COX1/2 inhibitor with potential anti-inflammatory activity in induced migraines, induced gastrointestinal injuries, and may be used in studies of increased intracranial pressure secondary to severe traumatic brain injury and rheumatoid arthritis in adults.

Indomethacin salicylate is an antiinflammatory drug. It has shown remarkable inhibitory effects on carrageenin edema, ultraviolet erythema and adjuvant arthritis.

Indomethacin acyl glucuronide, a metabolite of the COX inhibitor indomethacin (1), embodies an essential byproduct formed during the metabolic processing of indomethacin.

5-hydroxy Indomethacin is a metabolite of indomethacin .1It is formed from indomethacin in rabbit hepatic microsomes. 1.Evans, M.A., Papazafiratou, C., Bhat, R., et al.Indomethacin metabolism in isolated neonatal and fetal rabbit hepatocytesPediatr. Res.15(11)1406-1410(1981)

NO-indomethacin is a hybrid molecule of indomethacin and a nitric oxide (NO) donor. This drug design combines the anti-inflammatory properties of a non-steroidal anti-inflammatory drug (NSAID) with the gastrointestinal protective effects of NO. Compounds of this class retain their anti-inflammatory and analgesic activity, but have reduced gastrointestinal and kidney toxicity compared to the NSAID alone. NO-indomethacin also enhances the cancer chemopreventative activity of indomethacin. NO-indomethacin exhibits an IC50 of 82 μM, compared to >1,000 μM for indomethacin alone, for the inhibition of pancreatic cancer cell (PaCa-2) growth after 24 hours in culture.

BML-190 (Indomethacin morpholinylamide) is a specific CB2 receptor inverse agonist (Ki: 435 nM), with 50-fold selectivity over CB1 receptor.

Apyramide is an anti-inflammatory agent (NSAID) that acts as a prodrug of indomethacin, a potent, blood-brain permeable, and nonselective inhibitor of COX1 and COX2.

Tinoridine hydrochloride (Y-3642 hydrochloride) is a non-steroidal anti-inflammatory drug. Tinoridine hydrochloride (5-100 μM), produced a concentration-dependent inhibition on the simultaneous increases in lipid peroxide formation and renin release induced by 50 μM ascorbic acid in the renin granule fraction. On the other hand, indomethacin, hydrocortisone, and prednisolone, which had no ability to inhibit the lipid peroxidation in the renin granule fraction, did not influence the release of renin from the granules. These results suggest that tinoridine suppresses renin release by inhibiting the oxidative disintegration of membranes of renin granules.

MK 410 is an indomethacin analogue and anti-inflammatory agent that induces changes in the immune system by inhibiting plasma neutral protease activity.

Homopterocarpin and Pterocarpus extract offer gastroprotection against indomethacin- induced ulcer by antioxidative mechanism and the modulation of gastric homeostasis, homopterocarpin may be responsible for, or contribute to the antiulcerogenic property

Body Protection Compound 157 (BPC 157) is a pentadecapeptide derived from BPC, identified in gastric juice, exhibiting diverse biological activities. At 2 µg/ml, BPC 157 enhances primary rat tendon fibroblast cell migration and F-actin formation. Furthermore, doses of 0.01 and 10 µg/kg, intraperitoneally (i.p.), mitigate paw swelling, bone erosion, and mononuclear cell infiltration in the joints of rats with rheumatoid arthritis induced by complete Freund's adjuvant (CFA). It also diminishes gastric ulcer size in rats caused by indomethacin, aspirin, or diclofenac at these doses. Additionally, BPC 157 reduces catalepsy duration and tremor severity in a mouse model of Parkinson's disease triggered by MPTP.

COX-2 5-LOX-IN-1 (compound 3a), a benzothiophen-2-yl pyrazole carboxylic acid derivative, is a potent dual inhibitor of COX-2 and 5-LOX, exhibiting superior analgesic and anti-inflammatory properties compared to Celecoxib and Indomethacin. It demonstrates strong inhibitory activity against COX-1, COX-2, and 5-LOX, with IC50 values of 12.13 μM, 0.4 μM, and 4.96 μM, respectively [1].

16,16-dimethyl Prostaglandin E1 is a PGE1 (T1626) analog that induces bronchoconstriction and vascular smooth muscle contraction and inhibits indomethacin-induced cell elongation.

Ebopiprant, also known as OBE-022, is an Oral and Selective Prostaglandin F 2α Receptor Antagonist as an Effective and Safe Modality for the Treatment of Preterm Labor. OBE022 exhibits potent tocolytic effects on human tissues ex vivo and animal models in vivo without causing the adverse fetal side effects seen with indomethacin.

AHR-10037 is a nonsteroidal anti-inflammatory drug with analgesic and antipyretic properties as well as a high therapeutic index and low gastric toxicity. AHR-10037 was comparable to indomethacin in suppressing acute (Evans blue-carrageenan pleural effusion) and chronic (adjuvant-induced arthritis) inflammation. Studies have shown that it is converted in vivo to a prodrug of cyclooxygenase inhibitors.

COX-2 5-LOX-IN-2 is a benzothiophen-2-ylpyrazole carboxylic acid derivative that inhibits both COX-2 and 5-LOX. COX-2 5-LOX-IN-2 (5b) has IC50 values of 5.40, 0.01, and 1.78 μM for COX-1, COX-2, and 5-LOX, respectively, and exhibits greater analgesic and anti-inflammatory activities than Celecoxib and Indomethacin.

Acemetacin (TVX 1322) is a carboxymethyl ester of indometacin and a potent non-steroidal anti-inflammatory drug derived from indol-3-acetic acid, with its activity primarily attributed to its active metabolite, indomethacin. In clinical trials, acemetacin shows better gastric tolerability compared to indomethacin.

Isopulegol presents depressant- and anxiolytic-like effects, it also has anticonvulsant and bioprotective effects against PTZ-induced convulsions are possibly related to positive modulation of benzodiazepine-sensitive GABAA receptors and to antioxidant properties.Isopulegol presents significant gastroprotective effects in both ethanol- and indomethacin-induced ulcer models, which appear to be mediated, at least in part, by endogenous prostaglandins, K(ATP) channel opening, and antioxidant properties.