Lipoxygénase

Butibufen (FF-106) is a non-steroidal anti-inflammatory compound and LOX inhibitor with analgesic and antipyretic activity for the study of rheumatic diseases.

Applications The principal constitutents of frankincense (olibanum). A specific, nonredox inhibitor of 5-lipoxygenase used to treat inflammation. References Safayhi, H. et al.: J. Pharmacol. Exp. Therap., 261, 1143 (1992); Siemoneit, U., et al.: Eur. J. Pharmacol., 606, 246 (2009); Cao, H. et al.: Pharamacol. Res., 61, 519 (2010);

PF-4191834: Non-iron, non-redox 5-LOX inhibitor, IC50 = 229 nM, 300x selective over 12/15-LOX, inactive on COX enzymes.

Linoleyl alcohol (CIS,CIS-9,12-OCTADECADIENOL), fatty alcohol, is a structural analog of Linoleic acid with no a-carboxyl group[1].

ML355, a specific, effective 12-Lipoxygenase(12-LOX) inhibitors(IC50=0.34 μM), possess favorable ADME properties.

S-(+)-Marmesin (marmesin) is a coumarin originally isolated from the mature bark of A. marmelos,exhibiting COX-2/5-LOX dual inhibitory activity.

Applications Ketoconazole-d3 is the labeled analogue of Ketoconazole (K186000), which inhibits cytochrome P-450 dependent steps in the biosynthesis of steroid hormones in vivo. Antimetastatic and antineoplastic activity. Orally active 5-lipoxygenase and thromboxane synthase inhibitor. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Lambert, A., et al.: Biochem. Pharmacol., 35, 3999 (1986); Van Wauwe, J.P. and Janssen, P.A.J., J. Med. Chem., 32, 2231 (1989); Nardone, P.A., et al.: . Surg. Res., 44, 425 (1988); Tucker, W.F.G., et al.: Br. Med. J., 293, 882 (1986)

Ferroleuton is a selective competitive inhibitor of 5-lipoxygenase with an IC50 of 0.21 μM. It demonstrates antioxidant properties, clearing 86% of DPPH at 50 μM and exhibiting activities in ABTS (EC50 = 19.42 μM) and FRAP (EC50 = 3.32 μM) assays.

AZD 4407 is a potent inhibitor of 5-lipoxygenase.

Masoprocol (meso-Nordihydroguaiaretic acid) is a LOX inhibitor with anticancer and antihyperglycemic activity.

Tepoxalin (RWJ 20485), potential asthma and osteoarthritis drug, inhibits COX-1, COX-2, and 5-LOX with low IC50 values.

5-O-Demethylnobiletin is a natural anti-inflammatory that inhibits 5-LOX without altering COX-2 expression.

CJ-13,610 hydrochloride is an orally active nonredox-type inhibitor of 5-LOX and can be used in studies about the prevention of untoward pathophysiological

FPL 62064 is a potent dual inhibitor of 5-lipoxygenase (5-LOX) and COX (IC50 of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and prostaglandin

Diethylcarbamazine citrate treats filariasis, targeting W. bancrofti and L. loa by inhibiting arachidonic acid in microfilaria.

Applications An inhibitor of 5-lipoxygenase, the initial enzyme in the biosynthesis of leukotrienes from Arachidonic Acid. Used as an antiasthmatic. References Carter, G.W., et al.: J. Pharmacol. Exp. Ther., 256, 929 (1991), Weinblatt, M.E., et al.: J. Rheumatol., 19, 1537 (1992), McGill, K and Busse, W.W.: Lancet, 348, 519 (1996)

Aureusidin (Auresidin) shows antioxidant and lipoxygenase inhibitory activity with anti-inflammatory effects.

S-2474, an inhibitor of COX-2 and 5-lipoxygenase, has anti-inflammatory and neuroprotective activities, and inhibits cell death.

Lonapalene is a topically effective inhibitor of 5-lipoxygenase.