Indomethacin

Indomethacin (Indometacin) 是一种 COX1 和 COX2 抑制剂 (IC50=18 26 nM)，具有血脑屏障渗透性和非选择性。Indomethacin 是一种非甾体抗炎剂，具有抗肿瘤和抗感染活性。

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

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.

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.

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.

Indomethacin sodium hydrate (Indometacin sodium hydrate) 是一种口服活性、竞争性和可逆性的 COX1 2 抑制剂，具有潜在的抗炎活性，可诱发的偏头痛，诱导的胃肠道损伤，可用于研究成人继发于严重创伤性脑损伤的颅内压增高和类风湿性关节。

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)

Indomethacin farnesil (Infree) 是具有口服活性的 Indomethacin 前药，可通过干扰溶酶体的正常功能来破坏自噬流，有抗炎和抗风湿作用。它是一种可透过血脑屏障的，非选择性的 COX1和 COX2抑制剂，在 CHO 细胞中，对人 COX-1 和 COX-2 的IC50值分别为 18 nM 和 26 nM。

BML-190 (Indomethacin morpholinylamide) 是一种 CB2 受体的配体，其对 CB2 受体 (Ki:435 nM) 和 CB1受体 (Ki> 2 μM)。

Apyramide 是一种抗炎试剂 (NSAID)，是吲哚美辛的前药。Indomethacin 是一种强效的、血脑通透的、非选择性的 COX1 和 COX2 抑制剂。

Acemetacin (TVX 1322) 是一种非甾体抗炎类的化合物。

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。

AHR-10037是一种非甾体抗炎药，具有镇痛和解热特性以及高治疗指数，低胃毒性，它在抑制急性（伊文思蓝卡拉胶胸腔积液）和慢性（佐剂诱导的关节炎）炎症方面与吲哚美辛相当。研究表明，它在体内转化为环氧合酶抑制剂的前药。

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 是 PGE1 (T1626) 类似物，可诱导支气管收缩和血管平滑肌收缩，并抑制吲哚美辛诱导的细胞伸长。

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。

COX-2 5-LOX-IN-1 (compound 3a), a benzothiophen-2-yl pyrazole carboxylic acid derivative, is a potent and dual inhibitor of COX-2 5-LOX. It exhibits superior analgesic and anti-inflammatory properties compared to Celecoxib and Indomethacin. COX-2 5-LOX-IN-1 displays 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].

COX-2 5-LOX-IN-2 是苯并噻吩-2-基吡唑羧酸衍生物。COX-2 5-LOX-IN-2 (5b) 对COX-2和5-LOX 均有抑制作用。COX-2 5-LOX-IN-2 抑制 COX-1、COX-2 和 5-LOX 的IC50s 分别为 5.40、0.01 和 1.78 μM。COX-2 5-LOX-IN-2 显示出超过塞来昔布和吲哚美辛的镇痛和抗炎活性。

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.

11-Deoxy-11-methylene PGD2 (11d-11m-PGD2) 为 Prostaglandin D2 类似物，其结构中的 11-酮基由环外亚甲基替代。该化合物有效激活在 Indomethacin 存在下受到抑制的脂肪存储。

iNOS COX-2-IN-3(compound 7d)为iNOS与COX-2的双重抑制剂,展现出针对LPS诱导的RAW 264.7细胞的抗炎活性(IC50=3.48 μM).该化合物在血浆中表现出优良的稳定性,具备口服活性及良好的胃部耐受性,其对iNOS和COX-2的抑制效力分别是Indomethacin的5.43倍和2.37倍.