Metabolismo

<p>L-690488 has more effective cell penetration than L-690330. L-690488 is a prodrug of L-690330 and is a selective inositol monophosphatase (IMPase) inhibitor.</p>

<p>2-Myristyl dipalmitin (PMP), a triglyceride of palmitic acid, shows potential as a lipid marker for Wilson's disease (WD) [1] [2].</p>

<p>MS-444 (BE-34776) is an MLCK and HuR inhibitor with antitumor activity that can be used to study triple-negative breast cancer and colorectal cancer.</p>

<p>ICMT-IN-26 (compound 38) acts as an ICMT inhibitor with an IC50 value of 0.36 μM [1].</p>

<p>CMI-392 is a dual 5-lipoxygenase inhibitor and platelet-activating factor (PAF) receptor antagonist (IC50s: 100 and 10 nM).</p>

<p>1-Oleoyl-2-hydroxy-sn-glycero-3-PG (sodium salt), a lysophospholipid with oleic acid (18:1) at the sn-1 position, finds application in creating micelles, liposomes, and various artificial membranes, notably in lipid-based drug delivery systems.</p>

<p>Sulforhodamine 101 DHPE, a fluorescent probe, results from the conjugation of sulforhodamine 101, a red fluorescent dye with excitation/emission spectra of 586/605 nm, to the phospholipid 1,2-dipalmitoyl-sn-glycero-3-PE. It effectively integrates into phospholipid bilayers and is utilized for imaging solid supported lipid bilayers, detecting protein-ligand interactions on bilayers, and monitoring lipid probe colocalization in liposomes through resonance energy transfer (RET).</p>

<p>5,6-dehydro Arachidonic acid, an arachidonic acid analog with a 5,6 acetylene, inhibits 5-LO; Ki=15 μM in RBL cells, IC50=10 μM in guinea pig leukocytes.</p>

<p>IDH1 Inhibitor 7 is an IDH1 inhibitor with an IC 50 of less than 100 nM .</p>

<p>RORγt modulator 4 is a RORγt modulator that regulates IL-17A production activity in cells derived from mouse spleen.</p>

<p>ICMT-IN-22 (compound 62) acts as an ICMT inhibitor with an IC50 value of 0.63 μM [1].</p>

FTI-276 is an inhibitor of protein farnesyltransferase (PFT) (IC50s: 0.9 and 0.5 nM for Plasmodium falciparum and human).

<p>AS 183 is an inhibitor of cholesterol acyltransferase (ACAT).</p>

<p>MLS000545091 is a potent and selective human epithelial 15-lipoxygenase-2 mixed-type inhibitor.</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>Chinese gallotannin, a non-specific promiscuous inhibitor of α-amylase, exhibits a K(i) value of 0.82 μg/mL against human salivary α-amylase and shows potential</p>

<p>cis-ent-Tadalafil (cis-ent-IC-351) is a potent and selective PDE5 inhibitor that lowers blood pressure.</p>

<p>JTT 551: Selective PTP1B inhibitor for type 2 diabetes research; Ki=0.22μM for PTP1B, 9.3μM for TCPTP.</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>(+/-)12-HpETE, a vasodilator, is a 12-hydroxyicosatetraenoic acid produced by lipoxygenase [1].</p>

<p>Quizalofop-P, a selective herbicide, is absorbed by weed stems and leaves before translocating both upward and downward within the plant, concentrating in</p>

<p>First potent oral dual IDO1/IDO2 inhibitor with antitumor properties; IC50: 28 nM (IDO1), 144 nM (IDO2).</p>

<p>Bemoradan is an inhibitor of the rolipram-insensitive cyclic AMP phosphodiesterase from canine heart tissue</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>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.</p>

<p>BMS-185411 is a bio-active chemical.</p>

<p>3-Hydroxycarbofuran, a principal metabolite of Carbofuran, acts as a reversible inhibitor of acetylcholinesterase (AChE) [1].</p>

<p>Frunexian (EP-7041) is a selective and potent inhibitor of coagulation factor XI/activated factor XI, specifically targeting XIa.</p>

<p>Compound 105 (h15-LOX-2 inhibitor 1) is a potent inhibitor of human epithelial 15-lipoxygenase-2 (h15-LOX-2), exhibiting an IC50 of 0.34 μM [1].</p>

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

<p>Gentisuric acid, an Aspirin metabolite and a substrate of α-amidating monooxygenase (PAM), mitigates DNA damage induced by Mitomycin C. [1] [2]</p>

<p>C82 acts as an inhibitor of Mycobacterium tuberculosis (Mtb) cyclic dinucleotide phosphodiesterase (CdnP), with an IC50 value of 17.5 µM. This particular enzyme is responsible for breaking down cyclic di-AMP (c-di-AMP) into adenosine 5'-monophosphate (AMP). Notably, C82 demonstrates selectivity for Mtb CdnP over other bacterial cyclic dinucleotide phosphodiesterases (CDN PDEs) such as Yybt, RocR, and Group B Streptococcus (GBS) CdnP, as well as the mammalian CDN PDE ENPP1, and the viral CDN PDE poxin, showing effectiveness at a concentration of 200 µM.</p>

<p>GCase Modulator-1 (Compound 9g), a quinazoline derivative, functions as a glucosidase modulator with an AC50 value of 2.23 µM [1].</p>

<p>ICMT-IN-19 (compound 53) serves as a potent inhibitor of ICMT, demonstrating an IC50 value of 0.026 μM [1].</p>

<p>FAAH/cPLA2α-IN-1 is a compound that simultaneously inhibits both FAAH and cPLA2α, demonstrating potent activity with half-maximal inhibitory concentrations (</p>

<p>ICMT-IN-46 (compound 25) is a potent inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), exhibiting an IC50 value of 0.556 μM [1].</p>

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

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

<p>"Oral FXR antagonist 1 selectively blocks intestinal FXR, with IC50 of 2.1 μM, aiding in NASH research by improving liver health."</p>

<p>PPACK: synthetic peptide, irreversibly inhibits thrombin (Ki = 0.24 nM), prevents platelet activation.</p>

<p>Compound 144 (also known as Anticancer Agent 144) is a potent inhibitor of both PTPN2 and PTP1B, exhibiting IC50 values of less than 2.5 nM, making it suitable</p>

<p>1-Palmitoyl-2-oleoyl-sn-glycero-3-PA (1,2-POPA) is a phospholipid featuring a palmitic acid (16:0) chain that is saturated and an oleic acid (18:1) chain that is monounsaturated, positioned at the sn-1 and sn-2 locations, respectively. This compound is utilized in creating micelles, liposomes, and various artificial membrane forms.</p>

<p>Yonkenafil, a PDE5 inhibitor, may reduce stroke damage and aid in Alzheimer's treatment.</p>

Lp-PLA2-IN-2 is a selective and potent lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 0f 120 nM for recombinant human Lp-PLA2.

PF-04957325 is an inhibitor of PDE8.PF-04957325 has an IC50 of 0.7 nM for PDE8A.PF-04957325 can be used for the study of autoimmune encephalomyelitis.

<p>ICMT-IN-50 (compound 3) serves as an inhibitor of ICMT with an IC50 value of 0.31 µM [1].</p>

<p>MR-2-93-3, a long-chain fatty acid, functions as a carrier for polynucleotides [1].</p>

<p>Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are lipids recently discovered to be modulated by dietary influences such as fasting and high-fat feeding, and they play a role in enhancing insulin sensitivity. These compounds typically feature a carbon-16 or carbon-18 fatty acid (e.g., palmitoleic, palmitic, oleic, or stearic acid) esterified to a carbon-16 or carbon-18 hydroxy fatty acid. A specific example is 12-SAHSA, which consists of stearic acid linked to 12-hydroxy stearic acid. Notably, 12-SAHSA levels are found to be moderately increased in the serum of glucose tolerant AG4OX mice, a model characterized by adipose tissue-specific overexpression of the Glut4 glucose transporter.</p>