Metabolismo

<p>Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are endogenous lipids that are influenced by fasting and high-fat diets and linked to improved insulin sensitivity in mice. These compounds typically feature a chain of either 16 or 18 carbon atoms (for example, palmitoleic, palmitic, oleic, or stearic acid) esterified with a hydroxy fatty acid chain of similar length. One specific FAHFA, known as 5-OAHSA, consists of oleic acid bonded to the fifth carbon of hydroxy stearic acid. Within the FAHFA family, OAHSAs exhibit the highest serum levels in AG4OX mice, which are known for their glucose tolerance attributed to the overexpression of the Glut4 glucose transporter in adipose tissue.</p>

<p>ICMT-IN-23 (compound 36) serves as an inhibitor of ICMT, exhibiting a half-maximal inhibitory concentration (IC50) of 0.123 μM [1].</p>

<p>SHP2-IN-18 (compound 183) is a potent SHP2 inhibitor, exhibiting an IC50 of 3 nM and applicable to glioblastoma research [1].</p>

<p>Cis-13-Octadecenoic acid, a monounsaturated fatty acid, is identified in bovine milk fat.</p>

<p>ATX inhibitor 21 is a potent inhibitor of ATX (IC50: 3490 nM).</p>

15-PGDH-IN-1: potent oral 15-PGDH inhibitor, IC50=3nM, useful for tissue repair research.

<p>2-Myristyldistearin (SMS), a triacylglycerol comprising myristic acid and stearic acid [1], showcases its intricate structural composition.</p>

<p>8-Hydroxyguanine, generated through the oxidative degradation of DNA by the hydroxyl radical, serves as an indicator of oxidative stress in biological systems.</p>

<p>5-OP-RU is a MAIT-activating ligand, a major antigen of MAIT cells, a mucosal adjuvant, and can be used to study Mycobacterium tuberculosis infection.</p>

GSK2973980A is a selective Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) inhibitor (IC50: 3 nM).

<p>ICMT-IN-5 (compound 46) is an ICMT inhibitor with an IC50 value of 0.3 μM [1].</p>

<p>1a,1b-Dihomo Prostaglandin F2α (1a,1b-dihomo PGF2α), a hypothetical product of adrenic acid in the COX pathway, is predominantly synthesized in the renal medulla, reflecting the selective distribution of adrenic acid in this region.</p>

<p>9(Z),11(Z)-Octadecadienoic acid, an isomer of linoleic acid, demonstrates antitumor activity with an EC50 value of 446.1 µM [1].</p>

<p>Imiglitazar (TAK559) is a potent PPAR-β/δ receptor agonist with hypoglycemic effects.</p>

<p>II-B08 is a cell-permeable SHP2 inhibitor (IC50 = 5.5 µM). II-B08 blocks growth factor stimulated ERK1/2 activation and hematopoietic progenitor proliferation.</p>

<p>IDO1/2-IN-1 hydrochloride: Dual IDO1/2 inhibitor, IC50 of 28/144 nM, oral, with antitumor properties.</p>

<p>Raloxifene Bismethyl Ether hydrochloride is a Raloxifene metabolite and an estrogen receptor inactive compound on which both hydroxyl groups are absent.</p>

<p>S-Benzylglutathione acts as a competitive inhibitor of glutathionase and undergoes conversion by rat kidney microsomes into its cysteine derivatives.</p>

<p>C14-SPM, a branched-chain polyamine lipidoid, facilitates the delivery of siRNA [1].</p>

<p>Prostaglandin F2α-1-glyceryl ester undergoes oxidation via 15-hydroxyprostaglandin dehydrogenase (15-HPGDH) [1].</p>

<p>BMS-654457 is a small-molecule, reversible inhibitor of factor XIa (FXIa; Kis: 0.2 and 0.42 nM for human and rabbit FXIa).</p>

<p>WT IDH1 Inhibitor 2 blocks wild-type and R132H mutant IDH1 (IC50: 120 nM); related to GSK321.</p>

<p>DORI, a cationic lipid, efficiently delivers plasmid DNA in vitro, exhibiting lower cytotoxicity and high transfection efficiency [1].</p>

inhibitor of both glial and neuronal uptake of glutamate, aspartate and cysteate.

<p>MGAT2-IN-2 is a potent inhibitor of acyl CoA:monoacylglycerol acyltransferase 2 (MGAT2) (IC50 of 3.4 nM).</p>

<p>AR453588 hydrochloride is an orally bioavailable anti-diabetic glucokinase activator (EC50: 42 nM) with anti-hyperglycemic activity.</p>

<p>"(±)-2'-Hydroxy Ceramide (d18:0/18:0) is a sphingomyelin derivative isolated from mammalian platelets upon ADP stimulation [1]."</p>

<p>Magmas-IN-1 (compound 9), a small molecule Magmas inhibitor (SMMI), targets the mitochondria-associated granulocyte-macrophage colony-stimulating factor (GM-CSF</p>

<p>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.</p>

<p>ICMT-IN-37 (compound 41) serves as an inhibitor of ICMT with an IC50 value of 0.308 μM [1].</p>

<p>Safinamide acid, a potential impurity in commercial safinamide preparations and a degradation product of safinamide under thermal and oxidative stress, is encountered in the pharmaceutical formulation process.</p>

<p>1,2-Dilauroyl-sn-glycero-3-phospho-(2R)-glycerol is a type of phosphoglycerol characterized by the presence of lauric acid at the sn-1 and sn-2 positions. [Matreya, LLC. Catalog No. 1443]</p>

<p>ATX-001, an ionizable cationic lipid, is utilized in the creation of lipid nanoparticles (LNPs) for mRNA delivery [1].</p>

<p>PDE5-IN-2 is a potent, highly selective, and orally active inhibitor of PDE5(IC50 of 0.31 nM)</p>

<p>ICMT-IN-54 (compound 7c), an adamantyl analogue, serves as an ICMT inhibitor with an IC50 value of 12.4 μM, targeting the methylation process facilitated by</p>

<p>ICMT-IN-33 (compound 73) functions as an ICMT inhibitor with an IC50 value of 0.46 μM [1].</p>

<p>NOX2-IN-2 (compound 33) is a potent inhibitor of NOX2, disrupting the p47phox-p22phox protein-protein interaction with a dissociation constant (K i) of 0.24 μM.</p>

<p>RORγt Inverse agonist 6 is an agonist of RORγt inverse. RORγt Inverse agonist 6 can be used in research on Th17-driven autoimmune diseases.</p>

<p>SHP2-IN-19 (compound 183) is a SHP2 inhibitor exhibiting potent activity with an IC50 of 3 nM, and is utilized in glioblastoma research [1].</p>

<p>PDP-EA is an activator of fatty acid amide hydrolase(FAAH) and enhances the amidohydrolase activity of FAAH.</p>

<p>Niraxostat (Y-700) is one of the isocytosine derivatives as xanthine oxidase inhibitors.</p>

<p>MSI-1436 is a selective, non-competitive the enzyme protein-tyrosine phosphatase 1B (PTB1B)inhibitor(IC50 of appr 1 μM)</p>

<p>UK 357903, a phosphodiesterase 5A (PDE5A) inhibitor, is used potentially for the treatment of erectile dysfunction.</p>

<p>L-hydroxylysine dihydrochloride , is formed by posttranslational hydroxylation of some lysine residues. It is an amino acid, is exclusive to collagen protein.</p>

<p>MMV009085 is a potent inhibitor of the Plasmodium falciparum hexose transporter (Pf HT1), with potential as an anti-malarial agent.</p>

<p>5(S)-HETrE, made by 5-LO from mead acid, has unknown biological activity and metabolic fate.</p>

<p>Lp-PLA2-IN-9, a tetracyclic pyrimidinone, inhibits rhLp-PLA2 (pIC50: 10.1), promising for neurodegenerative research.</p>

<p>1,2-Dilinoleoyl-sn-glycero-3-PC (Dilinoleoyllecithin), a phospholipid, finds application in the production of artificial membranes [1].</p>

<p>Aladotril is an inhibitor of neutral endopeptidase. Its prodrug is aladotrilat.</p>

<p>ML395 is a potent, selective PLD2 allosteric inhibitor with potent antiviral activity (IC50 =360 nM).</p>