Métabolisme

4-epiMinocycline, recognized as a primary degradation product and a probable impurity in minocycline commercial formulations, is derived from minocycline, a broad-spectrum tetracycline antibiotic notable for its extended serum half-life. Besides treating acne, especially in older patients, minocylvania exhibits significant anti-inflammatory and neuroprotective effects.

C2 Dihydro Ceramide (d18:0/2:0) (C2 Dihydroceramide) is a ceramide that is a precursor of ceramide synthesis and stimulates ABCA1-mediated cholesterol efflux.

1,2-Dipalmitoyl-3-myristoyl-rac-glycerol, a triacylglycerol, incorporates palmitic acid at the sn-1 and sn-2 positions, along with myristic acid at the sn-3 position, and is identified in bovine milk fat.

N-Palmitoyl taurine, an amino-acyl endocannabinoid prominent in rat brain lipidomics profiling, accompanies multiple arachidonoyl amino acids isolated from bovine brain, including N-arachidonoylethanolamine (NADA) and N-arachidonoyl serine (ARA-S). Mass spectral lipidomic analysis of rat brain additionally revealed a series of fatty acyl amides with taurine. The function of N-Palmitoyl taurine is under investigation.

1-Palmitoyl-2-Linoleoyl-sn-glycero-3-phosphatidylcholine (PC) is a phospholipid characterized by the incorporation of palmitic (16:0) and linoleic (18:2) acids at the sn-1 and sn-2 positions, respectively. It is utilized in the creation of micelles, liposomes, and various artificial membranes, playing a significant role in research on lipid peroxidation.

1,2-Dioleoyl-3-lauroyl-rac-glycerol, a triacylglycerol, comprises oleic acid at the sn-1 and sn-2 positions and lauric acid at the sn-3 position. It is identified in the date seed oil and the fat body of male B. lapidarius bumblebees.

17(R)-Resolvin D3 (17(R)-RvD3) is an aspirin-triggered epimer of resolvin D3, produced from docosahexaenoic acid (DHA) through the action of COX-2 in the presence of aspirin, via a 17(R)-hydroperoxy DHA (17(R)-HDHA) intermediary. Identified in mouse inflammatory exudates, 17(R)-RvD3 notably inhibits the transmigration of isolated human polymorphonuclear cells (PMNs) and fosters the efferocytosis of apoptotic PMNs by macrophages. Furthermore, in a mouse model of zymosan-induced peritonitis, 17(R)-RvD3 administration (10 ng/animal) significantly curtails neutrophil infiltration into the peritoneal cavity and modulates cytokine levels by reducing IL-6 and increasing IL-10 in the inflammatory exudate. It engages GPR32, evidenced by activation in a β-arrestin reporter assay and augments phagocytosis more effectively in CHO cells overexpressing GPR32 compared to controls. Additionally, 17(R)-RvD3 enhances the clearance of etoposide-induced tumor cell debris by monocyte-derived macrophages in H460 human lung carcinoma.

Salbutamol (albuterol), a selective β2-adrenergic partial agonist, serves as a bronchodilator widely used in various clinical scenarios and to counteract doping abuse. Its process impurity, Albuterol methyl ether, may be present in urine samples, highlighting the importance of detection and chemical analysis.

6-Hydroxy Bexarotene, an oxidative metabolite of bexarotene, serves as a high-affinity ligand for retinoid X receptors (RXRs), specifically binding to RXRα, RXRβ, and RXRγ, as well as to the retinoic acid receptor α (RARα) with dissociation constants (Kds) of 3.46, 4.21, 4.83, and 8.17 μM, respectively. It demonstrates selective activation of RXRα, RXRβ, and RXRγ over RARα, RARβ, and RARγ in vitro, with half-maximal effective concentrations (EC50s) of 398, 356, 420, 4,414, 2,121, and 2,043 nM, respectively.

TRC160334 is a HIF hydroxylases inhibitor.

(R)-tert-OMe-byakangelicin, a furanocoumarin, exhibits inhibitory effects on liver drug metabolizing enzyme (DME) activity and can be isolated from the immature

4-Methylumbelliferyl-α-D-Glucopyranoside (4MU-αGlc) is a fluorescence substrate for α-glucosidase, serving as a biomarker for Fabry disease and Pompe disease

α-Glucosidase-IN-29 (compound 19) is an inhibitor of α-glucosidases, exhibiting an IC50 value of 1.21 μM and a Ki of 1.80 μM.

CETP-IN-3 is an inhibitor of the plasma glycoprotein cholesterol ester transfer protein (CETP), elevating HDL-C through inhibition of CETP.

A 79175 is a 5-lipoxygenase inhibitor that increases bone formation.

Sezolamide is a carbonic anhydrase inhibitor.

Bemfivastatin hemicalcium (PPD 10558), an orally active HMG-CoA reductase inhibitor, serves as a lipid-lowering agent.

PF-05236216 is a potent, selective, brain-penetrant CK1δ/ε inhibitor that modulates circadian rhythms in mice, supporting sleep and metabolic research.

S-(p-Nitrobenzyl)glutathione acts as a competitive inhibitor of glutathionase.

inhibitor of phosphodiesterase type 5 (PDE5)