Métabolisme

ICMT-IN-32 (compound 70) acts as an inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), demonstrating an IC50 value of 0.777 µM [1].

Zofenoprilat, an angiotensin-converting enzyme (ACE; IC50 = 8 nM for rabbit lung enzyme) inhibitor and the active metabolite of the prodrug zofenopril,

Dieicosanoin is a diacylglycerol that incorporates arachidic acid, a saturated long-chain fatty acid featuring a 20-carbon backbone. This acid is derivable from sources such as peanut butter and anaerobic fungi [1] [2].

Eprinomectin B1a, composing over 90% of the antiparasitic agent eprinomectin, is a primary component alongside eprinomectin B1b, which constitutes less than 10%. This compound is part of the avermectin family, used as insecticides and anthelmintics.

1,3-Dipalmitoyl-2-linoleoyl glycerol is a triacylglycerol featuring palmitic acid at the sn-1 and sn-3 positions, and linoleic acid at the sn-2 position. Identified within the palm stearin fraction of palm oil and as a trace constituent in soybean germ oil, this compound exemplifies the structural diversity of fats and oils in both plant-based sources.

GNE-6468 is a potent and selective agonist of RORγ(RORc) (EC50: 13 nM for HEK-293 cell).

Yonkenafil HCl, a PDE5 inhibitor, is used potentially for the treatment of erectile dysfunction.

1-Isopropyltryptophan (1-IsoPT), an IDO1 inhibitor, suppresses the expression of IDO-1 and IDO-2 mRNA induced by IFN-γ stimulation [1].

(±)13,14-EDT, an oxylipin metabolite derived from adrenic acid through the cytochrome P450 (CYP) pathway, acts as a potent activator of large-conductance

8(Z),14(Z)-Eicosadienoic Acid, an ω-8 C20:2 fatty acid, constitutes 0.19% of total fatty acids in human milk. In vivo, it is converted by desaturases into eicosatrienoic acids, known for their potent vasodilator properties. However, the physiological effects of 8(Z),14(Z)-Eicosadienoic Acid remain unexplored.

Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are recent discoveries in endogenous lipids that are influenced by dietary changes such as fasting and high-fat diets, showing a link with enhanced insulin sensitivity in mice. These compounds typically feature a C-16 or C-18 fatty acid (e.g., palmitoleic, palmitic, oleic, or stearic acid) bound to a hydroxy group on another C-16 or C-18 fatty chain. A specific FAHFA, 9-POHSA, consists of palmitoleic acid connected at the hydroxy stearic acid's 9th position. This molecule, in particular, exhibits notably increased levels in the serum of glucose-tolerant AG4OX mice, which express the Glut4 glucose transporter predominantly in their adipose tissue. Given the broader family of FAHFAs' roles in enhancing glucose tolerance, promoting insulin secretion, and exerting anti-inflammatory effects, 9-POHSA emerges as a potential bioactive lipid involved in managing metabolic syndrome and inflammation.

PHD-IN-1 (compound 80) serves as a potent PHD2 inhibitor, exhibiting an IC50 value of ≤5 nM.

Abiraterone sulfate N-oxide, a carboxylic acid and major metabolite of Abiraterone, is utilized in prostate cancer research [1] [2].

SMS1-IN-1 is a potent inhibitor of sphingomyelin synthase 1 (SMS1, IC50 = 2.1 μM), and can be used in the atherosclerosis studies.

AZD2716 is an effective selective phospholipase A2 inhibitor for the treatment of coronary artery and cardiovascular disease.

1,3-Dipalmitoyl glycero-2-phosphatidylethanolamine is a phospholipid incorporating saturated long-chain (16:0) stearic acid at the sn-1 and sn-3 positions, with phosphatidylethanolamine (PE) at the sn-2 position. Phosphatidylethanolamines, critical components of biological membranes, play essential structural and functional roles. Various PE types are instrumental in forming micelles, liposomes, and other synthetic membranes.

Iomazenil is an antagonist and partial inverse agonist of benzodiazepine and potential therapy for alcohol abuse.

Deleobuvir sodium (BI207127), a hepatitis C NS5B inhibitor, showed promise in some trials but was discontinued in 2013 due to insufficient efficacy.

IDO1/TDO-IN-6 (compound 11) is a dual inhibitor targeting IDO1 and TDO, exhibiting IC50 values of 2.25 μM for IDO1 and 2.89 μM for TDO.