Activators & Inhibitors

O-Desmethylangolensin (Legacy Tebubio ref. 282T37404). O-Desmethylangolensin, an intestinal bacterial metabolite of soybean sapogenins, possesses anticancer and antioxidant activities, and inhibits the proliferation of human breast cancer MCF-7 cells by inducing apoptosis and promoting cell cycle arrest.

Octanoyl Coenzyme A (sodium salt) (Legacy Tebubio ref. 282T37405). Octanoyl coenzyme A (octanoyl-CoA) is a medium-chain acyl CoA and a metabolic intermediate in mitochondrial fatty acid β-oxidation. Levels of octanoyl-CoA are increased in the liver of patients with Reye's syndrome and β-oxidation of octanoyl-CoA by medium-chain acyl CoA dehydrogenase (MCADH) is decreased in patients with MCADH deficiency (MCD). Octanoyl-CoA inhibits citrate synthase and glutamate dehydrogenase.

Apovincaminic acid hydrochloride salt (Legacy Tebubio ref. 282T37406). Apovincaminic acid hydrochloride salt, the primary active metabolite of Vinpocetine (VP), is orally active and has the ability to penetrate the brain. It demonstrates a neuroprotective mechanism of action [1][2].

Arachidonoyl-L-carnitine (chloride) (Legacy Tebubio ref. 282T37407). Carnitine facilitates the transport of fatty acids into the mitochondria to be used in fatty acid metabolism. It does so by accepting acyl groups from fatty acids complexed with coenzyme A, which yields esterified carnitine or acylcarnitines that enable the transport of fatty acyl groups into the inner mitochondrial matrix. β-Oxidation of fatty acids in mitochondria is inhibited by uncoupling conditions, thus changes in circulating levels of various acylcarnitines have been used to identify alterations in metabolic state.[1] [2] Arachidonoyl-L-carnitine formed from carnitine conjugated to arachidonic acid .

Bischloroanthrabenzoxocinone (Legacy Tebubio ref. 282T37408). Bacterial type II fatty acid synthesis (FAS-II) is mediated by a series of enzymes, each of which may be targeted by potential antibiotics. Bischloroanthrabenzoxocinone (BABX) is an inhibitor of FAS-II, blocking fatty acid synthesis in S. aureus and E. coli with IC50 values of 11.4 and 35.3 μg/ml, respectively. It inhibits the growth of S. aureus and permeable E. coli strains with minimum inhibitory concentrations ranging from 0.2-0.4 μg/ml. BABX also displays binding to liver X receptors (LXRs), inhibiting agonist binding in an LXRα-scintillation proximity assay (IC50 = 10 μM).

DPC-AJ1951 (trifluoroacetate salt) (Legacy Tebubio ref. 282T37409). DPC-AJ1951 is a peptide agonist of the parathyroid hormone (PTH)/PTH-related peptide receptor (PPR; EC50 = 0.15 nM in HEK293 cells expressing human PPR). It induces cAMP production in SAOS-2 and UMR106 cells that endogenously express human and rat PPR, respectively (EC50s = 2.2 and 1.1 nM, respectively). DPC-AJ1915 stimulates osteoclast-mediated bone resorption in fetal rat long-bone explant cultures and increases collagen synthesis and cell proliferation in neonatal mouse parietal bone explants.

(-)-borneol (Legacy Tebubio ref. 282T3741). (-)-borneol (L-Borneol) has a highly efficacious positive modulating action at GABA receptor with an EC50 of 237 μM.

9(R)-HETE (Legacy Tebubio ref. 282T37410). 9(R)-HETE, which constitutes 50% of (±)9-HETE, activates RXRγ-dependent transcription 1.5-fold relative to a control at a concentration of 300 nM. The stereochemical assignment of the (R) enantiomer is based on the comparison of chiral HPLC retention times to published results.

9(S)-HETE (Legacy Tebubio ref. 282T37411). 9(S)-HETE is an enantiomer which makes up 50% of (±)9-HETE . There are no reports of 9(S)-HETE occurring as an enzymatic lipoxygenation product. Whereas 12(S)-HETE promotes adhesion of several cell lines to endothelial cell monolayes, 9(S)-HETE and other positional HETEs are without effect. Stereochemical assignment of the (S) enantiomer is based on comparison of chiral HPLC retention times to published results.