Metabolism

9(Z),11(E)-Conjugated Linoleic Acid Methyl Ester, identified in lemon grass (C. flexuosus), serves as a standard for quantifying conjugated linoleic acids in thermally stressed olive oil and trans fats in bakery products. [Matreya, LLC. Catalog No. 1255]

KH064 is a sPLA2-IIA inhibitor of oral activity.

ZK824859 is an oral uPA inhibitor with IC50s: 79 nM (uPA), 1580 nM (tPA), 1330 nM (plasmin).

1,2-Dioleoyl-3-stearoyl-rac-glycerol, a triacylglycerol, features oleic acid at the sn-1 and sn-2 positions and stearic acid at the sn-3 position. This compound is present in sunflower, corn, and soybean oils, as well as in ostrich oil.

ICMT-IN-15 (compound 51) serves as an ICMT inhibitor with an IC50 value of 0.032 μM [1].

M5N36: selective Cdc25C inhibitor, IC50: 0.15µM A, 0.19µM B, 0.06µM C; halts cell growth, boosts p-CDK1/2.

2-Stearoyl-sn-glycero-3-phosphatidylcholine (2-Stearoyl-sn-glycero-3-PC) is a lysophospholipid characterized by the presence of stearic acid at the sn-2 position. This compound has been identified in the myocardium of rabbits.

PDE7-IN-3 (Example 2) serves as an inhibitor of phosphodiesterase PDE7 and exhibits potential analgesic properties.

sEH/AChE-IN-4-15 is a dual sEH and AChE inhibitor crossing the BBB, with IC50s: 3.1 nM (hsEH), 1660 nM (hAChE), 179 nM (hBChE), 14.5 nM (msEH), 102 nM (mAChE).

Monoacylglycerol lipase inhibitor 1, also known as compound 13 [1], is a potent inhibitor of monoacylglycerol lipase.

Palmitoleic acid, an ω-7 monounsaturated fatty acid found in macadamia and sea buckthorn oils, enhances both basal and insulin-stimulated glucose uptake, as well as Glut4 protein levels in 3T3-L1 adipocytes at a 200 µM concentration. Ex vivo, at a dosage of 300 mg/kg per day, it significantly increases glucose uptake and both aerobic and anaerobic glycolysis, while decreasing de novo fatty acid synthesis and the activity of lipogenic enzymes, specifically ATP citrate lyase (ACL) and glucose-6-phosphate dehydrogenase (G6PDH), in isolated murine adipocytes. Furthermore, the dietary administration of palmitoleic acid at 300 mg/kg mitigates high-fat diet-induced insulin resistance and liver inflammation in mice.

1-Linoleoyl-3-α-linolenoyl-rac-glycerol, a diacylglycerol, features linoleic acid at the sn-1 position and α-linolenic acid at the sn-3 position. This compound is identified in olive oil that has undergone lipase-catalyzed glycerolysis, utilizing immobilized lipase B derived from C. antarctica.

NUCC-0223619 is an IDO1 inhibitor that induces the degradation of IDO protein and can be involved in the synthesis of PROTAC.

Lignoceroyl ethanolamide, a fatty N-acyl ethanolamine within the endocannabinoid family, is derived from lignoceric acid, which is found in relatively high concentrations in rat cerebrospinal fluid. However, the specific function and significance of this metabolite remain unclear.

244cis, an ionizable cationic lipid incorporating a piperazine structure, facilitates the creation of lipid nanoparticles (LNPs). These LNPs, when formulated with 244cis and coated with an mRNA reporter gene, exhibit preferential accumulation in the lungs of mice, in contrast to those formulated with SM-102. Additionally, it leads to a reduction in the levels of serum chemokine (C-C motif) ligand 2 (CCL2) [1].

ATX inhibitor 15, an indole-based carbamate, has a 2.17 nM IC50 against ATX, suppresses pro-fibrotic genes, and protects against mouse lung fibrosis.

ICMT-IN-13 (compound 49) functions as an inhibitor of ICMT, exhibiting an IC50 value of 0.47 μM [1].

IDH1 Inhibitor 5 targets MOG cells (IC50: 64.4 nM) and R132H mutant IDH1 gliomas (IC50: 34.9 nM).

Homonojirimycin is an alpha-glucosidase inhibitor.

MγLnFP, an analog of methyl arachidonyl fluozophosphonate (MAFP), holds significance in pharmacological research due to its potential as an inhibitor of phospholipases, FAAH, and its role as a CB receptor ligand. However, the properties and effects of the γ-linolenyl variant of MAFP remain to be fully explored.