Metabolism

GSK2647544 inhibits Lp-PLA2, a pro-inflammatory enzyme from macrophages, orally active, calcium-independent.

NTE-122 is a competitive Acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor.

CKD-519: A CETP inhibitor with an IC50 of 2.3 nM, blocking cholesteryl ester transfer in serum.

CoPoP, a liposome-based vaccine adjuvant, holds potential for application in cancer research [1].

14,15-Epoxyeicosatrienoic acid (14,15-EET), derived from Arachidonic acid metabolism, significantly inhibits platelet aggregation in vivo and enhances

FXIa-IN-1 is a potent β-lactam covalent heparin-derived factor XIa (fXIa) inhibitor.

1-Myristoyl-2-linoleoyl-3-oleoyl-rac-glycerol, a triacylglycerol, features myristic acid, linoleic acid, and oleic acid at the sn-1, sn-2, and sn-3 positions, respectively. This compound is prevalent in mature human milk, infant formula fats, and butterfat.

FR-234938 is a non-nucleoside adenosine deaminase inhibitor with anti-inflammatory activity.

ICMT-IN-28 (compound 65) serves as an inhibitor of ICMT, exhibiting significant potency with an IC50 value of 0.008 μM [1].

PDE5-IN-42 is a selective inhibitor of second-generation phosphodiesterase type 5 (PDE5).

sEH/AChE-IN-3 -15: potent dual sEH & AChE inhibitor; crosses BBB; IC50: hsEH 0.4nM, hAChE 1.94nM, hBChE 615nM, msEH 4.3nM, mAChE 2.61nM.

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.

XR3054 is a farnesyl protein transferase inhibitor that blocks proliferation in certain cancer cells, not dependent on ras mutation status.

N-Oleoyl taurine, an amino-acyl endocannabinoid isolated from rat brain, along with several arachidonoyl amino acids such as N-arachidonoyl dopamine and N-arachidonoyl serine, have been derived from bovine brain. Mass spectral lipidomics analysis of rat brain revealed a series of fatty acyl amides of taurine, marking the discovery of a new class of compounds. These compounds, found in the kidney, are known to activate members of the transient receptor potential (TRP) family of calcium channels, with N-Oleoyl taurine specifically potentially activating TRPV1 and TRPV4 channels.

Metformin hydroxy analog 2, an oxidation product of the biguanide metformin (1), represents a chemically transformed variant of the original compound, showcasing a modified molecular structure through the process of oxidation.

CAXII-IN-1, antitumor, selectively inhibits CA XII with Ki of 3.8 nM for hCA XII and 56 nM for hCA IX.

ICMT-IN-29, also known as compound 66, effectively inhibits ICMT with an IC50 value of 0.019 μM [1].

secreted phospholipase A2 (sPLA2) inhibitor

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.

inhibitor of phosphodiesterase type 5 (PDE5)