||MDK36122, also known as H-PGDS Inhibitor I, is a Prostaglandin D Synthase (hematopoietic-type) Inhibitor. MDK36122 has no code name, and has CAS#1033836-12-2. The last 5-digit was used for name for easy communication. MDK36122 selectively blocks HPGDS (IC50s = 0.7 and 32 nM in enzyme and cellular assays, respectively) with little activity against the related human enzymes L-PGDS, mPGES, COX-1, COX-2, and 5-LOX.
||Tepoxalin, also known as ORF-20485; RWJ-20485; is a 5-lipoxygenase inhibitor potentially for the treatment of asthma, osteoarthritis (OA). Tepoxalin has in vivo inhibitory activity against COX-1, COX-2, and 5-LOX in dogs at the current approved recommended dosage.Tepoxalin inhibits inflammation and microvascular dysfunction induced by abdominal irradiation in rats. Tepoxalin enhances the activity of an antioxidant, pyrrolidine dithiocarbamate, in attenuating tumor necrosis factor alpha-induced apoptosis in WEHI 164 cells.
||Tenidap, also known as CP-66248, is a COX/5-LOX inhibitor and cytokine-modulating anti-inflammatory drug candidate that was under development by Pfizer as a promising potential treatment for rheumatoid arthritis, but Pfizer halted development after marketing approval was rejected by the FDA in 1996 due to liver and kidney toxicity, which was attributed to metabolites of the drug with a thiophene moiety that caused oxidative damage.
||PF-4191834 is a novel, potent and selective non-redox 5-lipoxygenase inhibitor effective in inflammation and pain. PF-4191834 exhibits good potency in enzyme- and cell-based assays, as well as in a rat model of acute inflammation. Enzyme assay results indicate that PF-4191834 is a potent 5-LOX inhibitor, with an IC(50) = 229 +/- 20 nM. Furthermore, it demonstrated approximately 300-fold selectivity for 5-LOX over 12-LOX and 15-LOX and shows no activity toward the cyclooxygenase enzymes. In addition, PF-4191834 inhibits 5-LOX in human blood cells, with an IC(80) = 370 +/- 20 nM.
||MK-886, also known as L 663536, is a leukotriene antagonist. It may perform this by blocking the 5-lipoxygenase activating protein (FLAP), thus inhibiting 5-lipoxygenase (5-LOX), and may help in treating atherosclerosis. MK-886 inhibits cyclooxygenase-1 activity and suppresses platelet aggregation. MK-886 induces changes in cell cycle and increases apoptosis after photodynamic therapy with hypericin. MK-886 enhances tumour necrosis factor-alpha-induced differentiation and apoptosis.
||L 691816 is a potent inhibitor of the 5-LO reaction both in vitro and in a range of in vivo models.
||CMI-977, also know as LPD-977 and MLN-977, is a potent 5-lipoxygenase inhibitor that intervenes in the production of leukotrienes and is presently being developed for the treatment of chronic asthma. CMI-977 inhibits the 5-lipoxygenase (5-LO) cellular inflammation pathway to block the generation of leukotrienes, which play a key role in triggering bronchial asthma.
||CJ-13610 is an orally active inhibitor of 5-lipoxygenase (5-LO) . CJ-13610 inhibits the biosynthesis of leukotriene B4 and regulates the IL-6 mRNA expression in macrophages. It is efficacious in preclinical models of pain.
||BRP-7 is a 5-LO activating protein (FLAP) inhibitor.