Results for Activators & Inhibitors ( 70846 )
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12-epi Leukotriene B4 (Legacy Tebubio ref. 282T37970). Leukotriene B4 (LTB4) compounds are produced by both enzymatic and non-enzymatic processes. The products of enzymatic origin, via Leukotriene A4 (LTA4) hydrolase, are stereospecifically 12(R). Non-enzymatic hydrolysis products are 50:50 mixtures at C-12, but are almost exclusively trans at C-6. Thus, the non-enzymatic hydrolysis product of LTA4 is 6-trans-12-epi LTB4. 12-epi LTB4 is an isomer which would not be expected to occur in either non-enzymatic hydrolysis products, or in the enzymatic products of LTA4 hydrolase. Compared to LTB4, 12-epi LTB4 has significantly reduced activity for the LTB4 receptor on human neutrophils (IC50 of 7.5 mM), and on guinea pig lung membranes with a (Ki of 4.7 mM). 12-epi LTB4 is an weak agonist at both the recombinant human BLT1 and BLT2 receptors, requiring approximately 10 mM for full activation of the receptor.
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12-OxoETE (Legacy Tebubio ref. 282T37972). 12-OxoETE is synthesized by human platelets and Aplysia nervous tissue after incubation with arachidonic acid. Microsomal fractions of various tissues will reduce 12-oxoETE to 12(S)-HETE or a mixture of 12(S)- and 12(R)-HETE. 12-OxoETE induces a rapid, dose dependent increase of cytoplasmic free calcium via a leukotriene B4 receptor or a common activation sequence.
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13(R)-HODE (Legacy Tebubio ref. 282T37973). 13(R)-HODE is the opposite enantiomer of 13(S)-HODE produced when linoleic acid is incubated with soybean lipoxygenase. Its presence in supernatants and membranes of cultured bovine endothelial cells has been attributed to COX metabolism. 13(R)-HODE is a weak (IC50 = 2.7 μM) inhibitor of U-46619-induced platelet aggregation.
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(S)-Coriolic acid (Legacy Tebubio ref. 282T37974). (S)-Coriolic acid (13(S)-HODE) is an important intracellular signaling agent generated by the reaction of linoleic acid with plant and mammalian lipoxygenases. It is involved in cell proliferation and differentiation in various biological systems and inhibits the adhesion of tumor cells to the vascular endothelium, while down-regulating IRGpIIb/IIIa receptor expression at around 1 μM. Additionally, (S)-Coriolic acid is a metabolite of 15-lipoxygenase (15-LOX) and often acts as an endogenous ligand to activate PPARγ. It induces mitochondrial dysfunction and airway epithelial damage.
13(S)-HODE-biotin (Legacy Tebubio ref. 282T37975). 13(S)-HODE is the lipoxygenase metabolite of linoleic acid. 13(S)-HODE modulates the platelet-activating factor, leukotriene B4, and formyl-Met-Leu-Phe-induced calcium influx in human polymorphonuclear leukocytes. The mechanism by which 13(S)-HODE elicits its inhibitory effect is still unclear. The use of biotinylated 15(S)-HETE as a probe for detecting binding proteins and/or receptors that specifically bind 15(S)-HETE provides a basis for similar use of 13(S)-HODE-biotin.