no indomethacin

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 heptyl ester 是 COX-1 和 COX-2 的非选择性抑制剂。

O-Desmethyl-N-deschlorobenzoyl indomethacin is a metabolite of the non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor indomethacin .1It is 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.2It has also been used in the synthesis of prostaglandin D2receptor antagonists.3 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) 2.Morgan, A.G.M., Babu, D., Michail, K., et al.An evaluation of myeloperoxidase-mediated bio-activation of NSAIDs in promyelocytic leukemia (HL-60) cells for potential cytotoxic selectivityToxicol. Lett.28048-56(2017) 3.Torisu, K., Kobayashi, K., Iwahashi, M., et al.Discovery of new chemical leads for prostaglandin D2 receptor antagonistsBioorg. Med. Chem. Lett.14(17)4557-4562(2004)

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)

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 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.

COX-2-IN-51 (E25) 是一种高效的COX-2抑制剂，IC50为70.7 nM。它显著抑制LPS诱导的NO和PGE2释放，并减少COX-2和iNOS的表达，以及抑制NF-κB通路激活。在多种小鼠模型中，通过抑制NF-κB通路，COX-2-IN-51展示了抗炎和镇痛特性。此外，其胃肠道副作用比Indomethacin更低。

Tinoridine hydrochloride (Y-3642 hydrochloride) 是非甾体抗炎药，具有显著的自由基清除和抗过氧化物特性。