Metabolismo

<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>RORγt agonist 3 is a potent agonist of RORγt.</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>BMS-986172 is an orally active, highly selective inhibitor of MGAT2, demonstrating inhibitory concentrations (IC50) of 4.6 nM for human MGAT2 (hMGAT2) and 20 nM</p>

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

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

<p>cis-Clopidogrel-MP derivative, also Clopidogrel-MP-AM, is a 3'-methoxyacetophenone Clopidogrel metabolite and oral P2Y12 receptor platelet inhibitor.</p>

<p>VU0364739, a selective phospholipase D2 (PLD2) inhibitor with an IC50 of 22 nM, effectively reduces cancer cell proliferation [1].</p>

<p>AS 183 is an inhibitor of cholesterol acyltransferase (ACAT).</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>HIF-2α-IN-13 (18) acts as a HIF-2α inhibitor and exhibits an IC 50 value of 2.7 μM.</p>

hCAIX-IN-16 (Compound 12d), an inhibitor of hCA IX, exhibits inhibition constants (K i) of 190.0 nM for hCA IX and 187.9 nM for hCA XII.

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

<p>Perindopril acyl-β-D-glucuronide is a metabolite of the ACE inhibitor perindopril [1].</p>

<p>PPARδ agonist 9 (compound 21), with an EC50 of 3.6 nM, is effective in vivo, decreasing serum MCP-1 concentrations in mice and markedly reducing atherosclerotic</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>ICMT-IN-33 (compound 73) functions as an ICMT inhibitor with an IC50 value of 0.46 μM [1].</p>

<p>Darodipine (PY-108068) is a dihydropyridine type Ca+2 antagonist.</p>

<p>9-OxoODE, formed through the oxidation of the allylic hydroxyl group in both 9(S)-HODE and 9(R)-HODE, is present in rabbit reticulocyte plasma and mitochondrial membranes as both 9- and 13-oxoODEs, constituting approximately 2% of the total linoleate residues. The majority of these oxidized linoleate residues are esterified to membrane lipids.</p>

<p>D-threo-PDMP inhibits glucoceramide synthase, cutting cell surface glycosphingolipids and hindering neurite growth.</p>

<p>hMAO-B-IN-32 is a potent hMAO-B selective inhibitor with an IC50 of 45.52 μM.</p>

<p>11β-13,14-Dihydro-15-keto PGF2α, a PGD2 metabolite in the 15-hydroxy PGDH pathway, is formed in human males upon infusion or inhalation of tritiated PGD2, with peak plasma levels of both 11β-PGF2α and 11β-13,14-dihydro-15-keto PGF2α observed within 10 minutes. In human lung homogenates, PGD2 is metabolized firstly to 11β-PGF2α and subsequently to 11β-15-keto-PGF2α in the presence of NAD+, but not to 11β-13,14-dihydro-15-keto PGF2α. Conversely, guinea pig liver and kidney homogenates can metabolize PGD2 to 11β-13,14-dihydro-15-keto PGF2α via 11β-PGF2α, with both NAD+ and NADP+ being requisite for this conversion.</p>

<p>Fatty acid amide hydrolase (FAAH), an enzyme responsible for the hydrolysis and inactivation of fatty acid amides like anandamide and oleamide, has been identified as a target by the potent FAAH inhibitor PHOP. PHOP demonstrates remarkable inhibitory activity with K_i values as low as 0.094 nM for human FAAH and 0.2 nM for rat FAAH. Additionally, through a proteomics assay focusing on the serine hydrolase enzyme family, to which FAAH belongs, PHOP's selectivity was evaluated, presenting IC_50 values of 1.1 nM against FAAH, 1.4 nM against triacylglycerol hydrolase (TGH), and greater than 100 µM against an uncharacterized hydrolase (KIAA1363). This specificity profile of PHOP underscores its potential for yielding precise outcomes in studies involving complex biological systems.</p>

<p>Efipladib is a phospholipase inhibitor. Efipladib decreases nociceptive responses without affecting PGE2 levels in the cerebral spinal fluid.</p>

<p>Gisadenafil (UK-369003) is a selective inhibitor of phosphodiesterase 5 (PDE5) with an IC50 of 3.6 nM and prevents degradation of cGMP.</p>

<p>DGAT1-IN-1 is a potent inhibitor of diacylglycerol O- acyltransferase type 1(DGAT1, IC50 of &lt; 10 nM).</p>

<p>PDE12-IN-3 is an inhibitor of phosphodiesterase 12 (PDE12) (pXC50 of 7.68),with antiviral activity.</p>

<p>7-BIA is a receptor-type protein tyrosine phosphatase D (PTPRD) inhibitor with anti-addictive properties and can be used in the study of neuropathic pain.</p>

<p>CCT365623: oral Lysyl Oxidase inhibitor, potent, selective, good pharmacokinetics, anti-metastatic.</p>

<p>NEP-IN-1 is an inhibitor of neutral endopeptidase (NEP, IC50 = 2 nM) and can be used in studies about female sexual arousal disorders.</p>

<p>Cis-22a: selective TRPV6 inhibitor (IC50=0.32μM), halts T47D breast cancer cell growth.</p>

<p>Ecopladib inhibits cPLA2α with IC50 of 0.15 μM (micelles) &amp; 0.11 μM (rat blood).</p>

<p>Fluspirilene is a long-acting antipsychotic for schizophrenia, inhibiting L-type calcium channels (IC50: 0.03 μM).</p>

<p>h-NTPDase-IN-2 is a broad-spectrum NTPDase inhibitor that inhibits multiple h-NTPDas isoforms.</p>

<p>WAY-620147 inhibits Monoamine Oxidase and can be used for the study of neurological disorders.</p>

HIF-2α agonist 2 is an HIF-2α agonist with an EC50 value of 1.68 μM for HIF-2α.

<p>Xanthine oxidase-IN-1 is an effective inhibitor of xanthine oxidase with an IC50 value of 6.5 nM.</p>

<p>Enpp-1-IN-16 is an ENPP1 inhibitor, yo anti-cancer activity.Enpp-1-IN-16 can be used to study insulin resistance and chondrocalcinosis.</p>

<p>PXS-6302 hydrochloride is a potent irreversible lysine oxidase (LOX) inhibitor, inhibiting Bovine LOX, rh LOXL1, rh LOXL2, rh LOXL3, and rh LOXL4 with IC50 of 3</p>

<p>ER-50891 is a potent RARα antagonist, countering retinoic acid inhibition and aiding BMP2-induced osteoblast differentiation.</p>

<p>Setileuton (MK0633) is a specific 5-LOX inhibitor and can be used in research on asthma and atherosclerosis.</p>

<p>Dechloro Rivaroxaban is a Factor Xa inhibitor that inhibits free FXa and plasminogen and fibrin-associated FXa activity in humans.</p>

<p>4A3-SC8 is a modular, degradable dendrimer facilitating the extension of survival in aggressive liver cancer models through the delivery of small RNAs [1].</p>

<p>ALDH2 modulator 1 is a potent and orally active modulator of acetaldehyde dehydrogenase-2 (ALDH2), which reduces blood alcohol levels in mice.</p>

<p>KB-74935: enzyme inhibitor, mineralocorticoid blocker, treats cholesterol, hypolipidemia, neurological issues, Alzheimer's.</p>

<p>AMG 579 is an efficacious and selective inhibitor of PDE10A (IC50 = 0.1 nM).</p>

<p>Calcium channel-modulator-1 is a calcium channel-modulator (IC50:0.8 μM) with specialisation to block aortic constriction.</p>

<p>PA452 is a selective antagonist of retinoic X receptor (RXR) and suppresses the effect of Retinoic acid on Th1/Th2 development.</p>