indomethacin

Indomethacin is an orally active nonsteroidal anti-inflammatory drug (NSAID) that non-selectively inhibits cyclooxygenase enzymes COX-1 and COX-2, with IC₅₀ values of 18 nM and 26 nM, respectively. It exhibits good blood-brain barrier permeability and shows significant anti-inflammatory, anti-tumor, and anti-infective activities. Indomethacin is widely used in research related to cancer, inflammation, and viral infections, and is also commonly used to induce gastric ulcer models in animals.

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

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.

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.

Indomethacin-D4 is a deuterium labeled Indomethacin. Indomethacin (T0458) 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.

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-D4 (Standard) is a reference standard of Indomethacin-D4 intended for quantitative analysis, quality control, and related biochemical research applications. 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.

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

Indomethacin sodium is a potent and orally active COX-1/2 inhibitor with IC50 values of 18 nM and 26 nM, respectively. It possesses anti-inflammatory, anticancer, and anti-infective activities and is widely used in research on cancer, inflammation, and viral infections. Additionally, it can be used to establish gastric ulcer animal models.

Indomethacin sodium hydrate is an effective orally active, competitive, and reversible inhibitor of COX-1 and COX-2, with IC50 values of 18 nM and 26 nM, respectively. It possesses anti-inflammatory, anticancer, and antimicrobial activities and is commonly used in research related to cancer, inflammation, and viral infections. Additionally, it can induce migraines and gastrointestinal injury and is used to study increased intracranial pressure secondary to severe traumatic brain injury in adults, as well as rheumatoid arthritis. It can also be used to induce gastric ulcer models.

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.

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)

N-Deschlorobenzoyl indomethacin is the primary metabolite of indomethacin, exhibiting very weak inhibitory activity against AKR1C2 (IC50=100 μM) and AKR1C3 (IC50>100 μM).

Indomethacin-D4 Methyl Ester is the deuterated form of Indomethacin Methyl Ester (T65290). Indomethacin (Indometacin) serves as a potent, non-selective inhibitor of COX-1 and COX-2 that can cross the blood-brain barrier, with IC50 values of 18 nM for COX-1 and 26 nM for COX-2 in CHO cells. It disrupts autophagic flux by interfering with the normal function of lysosomes.

Indomethacin-[13C6] (Standard) is a reference standard of Indomethacin-[13C6] intended for quantitative analysis, quality control, and related biochemical research applications.

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.

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.

COX-2-IN-51 (E25) is a potent COX-2 inhibitor with an IC50 of 70.7 nM. It significantly suppresses LPS-induced release of NO and PGE2, the expression of COX-2 and iNOS, and the activation of the NF-κB pathway. Displaying anti-inflammatory and analgesic effects in various mouse models through NF-κB pathway inhibition, COX-2-IN-51 has lower gastrointestinal side effects compared to 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.

Difenpiramide is a non-steroidal anti-inflammatory drug (NSAID) related to the research of degenerative and inflammatory arthropathies. Research shows Difenpiramide demonstrated anti-inflammatory effects comparable to indomethacin and phenylbutazone, with additional peripheral analgesic, antipyretic, and uricosuric activities. Difenpiramide inhibits prostaglandin synthesis and inflammatory mediators without affecting platelet aggregation or coagulation, and its therapeutic index was found to be more favorable than reference NSAIDs.

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

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

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.