Sigma-Aldrich 12/15-Lipoxygenase Inhibit

Assay

≥97% (HPLC)

Quality Level

100

Form

powder

Manufacturer/Tradename

Calbiochem^®

Storage Condition

OK to freeze
protect from light

Color

yellow

Solubility

DMSO: 100 mg/mL

Storage Temp.

2-8°C

General Description

A cell-permeable, non-toxic naphthyl-oxazole compound that acts as a highly potent, selective, active site directed, mixed type inhibitor of lipoxygenase-12/15 (IC₅₀= 200 nM for human). The inhibition appears to be non-reductive and reversible in nature. Displays excellent selectivity over 5-LOX (IC₅₀>50 µM), 12-LOX (IC₅₀>100 µM), and 15-LOX (IC₅₀>100 µM) and does not affect the activity of COX-1 and -2 in any significant manner (<10% inhibition at 15 µM). Can cross the blood brain barrier (brain to plasma ratio = 2.8). Offers protection against glutamate-induced oxidative toxicity in mouse neuronal HT22 cells and reduces the size of infarcts in a murine model of ischemic stroke. Displays good aqueous stability over a wide range of pH. Exhibits attractive pharmacokinetic properties (t_1/2~ 1 H in both plasma and brain; C_maxof 13.8 and 28.8 µM in plasma and brain, respectively; at 30 mg/kg, i.p).A cell-permeable, non-toxic naphthyl-oxazole compound that acts as a highly potent, selective, active site directed, mixed type inhibitor of lipoxygenase-12/15 (IC₅₀= 200 nM for human). The inhibition appears to be non-reductive and reversible in nature. Displays excellent selectivity over 5-LOX (IC₅₀>50 µM), 12-LOX (IC₅₀>100 µM), and 15-LOX (IC₅₀>100 µM) and does not affect the activity of COX-1 and -2 in any significant manner (<10% inhibition at 15 µM). Can cross the blood brain barrier (brain to plasma ratio = 2.8). Offers protection against glutamate-induced oxidative toxicity in mouse neuronal HT22 cells and reduces the size of infarcts in a murine model of ischemic stroke. Displays good aqueous stability over a wide range of pH. Exhibits attractive pharmacokinetic properties (t_1/2~ 1 H in both plasma and brain; C_maxof 13.8 and 28.8 µM in plasma and brain, respectively; at 30 mg/kg, i.p).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Biochem/Physiol Actions

Cell permeable: yesPrimary Target
12/15-LOXReversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Rai, g., et Al. 2014.J. Med. Chem. 57,4035.CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany