Metabolismo

<p>Arachidonoyl amide (AMC-AA) is a fatty acid amide among several that serve to quantify fatty acid amide hydrolase (FAAH) activity. FAAH, with its relative lack of selectivity, processes various amide head groups beyond ethanolamine, the head group of its primary endogenous substrate, anandamide (AEA). The interaction of AMC-AA with FAAH leads to the liberation of fluorescent aminomethyl coumarin, which has an absorption peak at 360 nm and emission at 465 nm. This fluorescence release facilitates the rapid and efficient assessment of FAAH activity through the utilization of either a standard cuvette or a microplate fluorometer.</p>

<p>LY-338979 is an impurity of pemetrexedone.</p>

<p>PF-915275 inhibits 11βHSD1 in humans (Ki=2.3 nM, EC50=15 nM) and affects cortisone-cortisol conversion in hepatocytes.</p>

<p>cKK-E15, a peptide-lipid, is instrumental in formulating LNP3 alongside C14PEG2000, unmodified cholesterol, and DOPE [1].</p>

<p>4BAB (compound 29) is an irreversible inhibitor of glyoxalase I (GLO1) and exhibits anticancer activity.</p>

<p>VU0155069 hydrochloride (CAY10593 hydrochloride) is a potent and selective inhibitor of phospholipase D (PLD), exhibiting IC50 values of 46 nM for PLD1 and 933 nM for PLD2. It effectively inhibits the migration of both human and mouse breast cancer cell lines [1] [2].</p>

<p>6β-hydroxy Testosterone （4-Androsten-6β,17β-diol-3-one） is a 17β-hydroxy steroid, an androgen and endogenous metabolite.</p>

<p>YG1702, a potent inhibitor specific to ALDH18A1, suppresses the proliferation of MYCN-amplified neuroblastoma (NB) and reduces MYCN expression.</p>

<p>JTT 551: Selective PTP1B inhibitor for type 2 diabetes research; Ki=0.22μM for PTP1B, 9.3μM for TCPTP.</p>

<p>CAY10435, a β-ketooxazapyridine and selective FAAH inhibitor, exhibits antimicrobial properties. It binds non-competitively to the FAAH of Dictyostelium discoideum, demonstrating a Kd value of 0.57 nM [1] [2].</p>

<p>Sch59498 is a potent phosphodiesterase 1c (Pde1c) inhibitor.</p>

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

<p>Leukotriene C4 (14,15-LTC4) is an inflammatory mediator synthesized from arachidonic acid through the actions of 15- and 12-lipoxygenases (LOs), involving intermediates such as 15-HpETE and 14,15-LTA4. Unlike the majority of leukotrienes formed via the 5-LO pathway, 14,15-LTC4 is an eoxin predominantly produced by eosinophils, although mast cells and nasal polyps can also synthesize it. While its physiological roles are not well understood, 14,15-LTC4 exhibits limited contractile activity on guinea pig ileum and pulmonary parenchyma. However, it can increase vascular permeability in human endothelial cell monolayers in vitro with potency comparable to 5-LO-derived leukotrienes, contributing to plasma leakage characteristic of inflammation.</p>

<p>ZK824190: oral uPA inhibitor, IC50 - uPA 237 nM, tPA 1600 nM, Plasmin 1850 nM.</p>

<p>Potent CETP inhibitor, boosts HDL-C levels, orally active; IC50=4nM.</p>

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

<p>Amb123203 is an inhibitor of the budding of mVP40 and eVP40 VLPs that acts by blocking mVP40-795 Nedd4 protein-protein interaction.</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>L-869298 is a potent and selective inhibitor of PDE4.</p>

<p>PPARγ agonist 8, a compound that acts on the peroxisome proliferator-activated receptor gamma (PPARγ), has been shown to stimulate peroxisome proliferator</p>

<p>(+/-)12-HpETE, a vasodilator, is a 12-hydroxyicosatetraenoic acid produced by lipoxygenase [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>GPX4-IN-2 is a potent inhibitor of GPX4, exhibiting antiproliferative activity. It holds potential for cancer research applications.</p>

<p>9(Z),11(E),13(Z)-Octadecatrienoic acid methyl ester, an isomer of 9(Z),11(E),13(E)-octadecatrienoic acid methyl ester and the methyl ester derivative of 9(Z),11(E),13(Z)-octadecatrienoic acid, serves as a standard for quantifying 9(Z),11(E),13(Z)-octadecatrienoic acid in wild growing pomegranate (P. granatum) seed oil [Matreya, LLC. Catalog No. 1240].</p>

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

<p>M-0002, a vasopressin V2 receptor antagonist, is used potentially for the treatment of ascites.</p>

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

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

<p>ICMT-IN-47 (compound 26) acts as an ICMT inhibitor with an IC50 value of 0.76 μM [1].</p>

<p>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].</p>

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

<p>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.</p>

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

<p>MK-8245 analog is an analog of MK-8245 which is a liver-targeted Inhibitor of Stearoyl-CoA Desaturase (SCD).</p>

<p>1-Stearoyl-2-hydroxy-sn-glycero-3-PG, a lysophospholipid characterized by the presence of stearic acid (18:0) at the sn-1 position, finds application in the creation of micelles, liposomes, and various artificial membranes, including those utilized in lipid-based drug delivery systems.</p>

<p>15-PGDH-IN-2 (Compound 2) is an inhibitor of 15-PGDH with an IC50 value of 0.274 nM. This compound is useful for research into hair loss, bone formation, gastric ulcer healing, and dermal wound healing [1].</p>

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

<p>ICMT-IN-7 (compound 74), with an IC50 value of 0.015 µM, functions as an ICMT inhibitor, promotes cytoplasmic accumulation of ICMT in HCT-116 cells in a dose-</p>

<p>B 581 is an inhibitor that specifically blocks farnesylated.</p>

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

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

<p>Pentadecanoyl ethanolamide, a derivative of the endogenous lipid amides (N-acylethanolamines), demonstrates anticonvulsant efficacy in electroshock-induced seizures in mice, exhibiting minimal toxicity [1].</p>

<p>DC271, a retinoid and RAR agonist, mimics the cellular effects of the endogenous ATRA and the synthetic EC23, by binding to retinoid protein machinery such as CRABPII to facilitate the translocation of ATRA into the nucleus [1].</p>

<p>ICMT-IN-43 (compound 22) acts as a potent inhibitor of the enzyme ICMT, exhibiting an inhibitory concentration (IC50) value of 0.04 μM [1].</p>

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

<p>15-beta PGF2α, a biochemical compound, serves as a pivotal mediator in diverse physiological processes.</p>

<p>AZD6605 is a potent, reversible inhibitor of, MMP2, MMP9, MMP12 and MMP13.</p>

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

<p>JNJ-42259152 is a phosphodiesterase 10A PET tracer.</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>