Metabolismo

<p>CRX000227 is a PPAR modulator suitable for researching metabolic and cell proliferative disorders [1].</p>

<p>Mitochondria degrader-1, a potent autophagy inducer, aids in neurodegenerative, cancer, and aging disease research.</p>

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

<p>Miglustat hydrochloride (N-Butyldeoxynojirimycin hydrochloride) is an inhibitor of glucosylceramide synthase and can be used for studies about Type I Gaucher</p>

<p>glycogen phosphorylase inhibitor</p>

<p>H2-003 is a selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2).</p>

<p>C12-113, a lipidoid delivery agent, effectively transfects siRNA into cells and, when combined with additional lipids, forms lipid nanoparticles (LNPs). These LNPs facilitate the delivery of mRNA encoding the spike glycoprotein of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in mice [1] [2].</p>

<p>ICMT-IN-34 (compound 39) serves as an effective inhibitor of ICMT, exhibiting an IC50 value of 0.17 μM [1].</p>

<p>ICMT-IN-18 (compound 35) serves as an ICMT inhibitor with an IC50 value of 0.066 μM [1].</p>

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

<p>BMS-986318: potent FXR agonist, EC50=53/350 nM, good ADME, effective in liver disease models, for nonalcoholic steatohepatitis research.</p>

<p>MK-0736 is a potent and selective 11β-HSD-1 inhibitor.</p>

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

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

<p>Compound 1e, also known as ALP/Carbonic anhydrase-IN-1, is a dual inhibitor targeting both carbonic anhydrase (CA) isozymes II, IX, and XII, as well as alkaline</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>DLPA is a phosphatidic acid (PA) that incorporates the medium-chain lauric acid (12:0).</p>

<p>LFHP-1c, a neuroprotective PGAM5 inhibitor, demonstrates efficacy in preserving blood-brain barrier integrity following ischemic stroke.</p>

<p>Ilepatril, also known as AVE-7688, is a vasopeptidase inhibitor for the treatment of hypertension.</p>

<p>Prostaglandin B2 is a dehydration product of PGE2/PGA2 with weak TP receptor activity, raising rabbit pulmonary pressure at &gt;5 ug/kg.</p>

<p>FXIa-IN-7 is an orally available, selective and potent inhibitor of factor XIa for the study of thrombophilia.</p>

<p>ICMT-IN-36 (compound 40) serves as an ICMT inhibitor, with an IC50 value of 0.181 μM [1].</p>

BAY-7081 is a cyanopyridone-based compound that functions as a potent, selective, and orally active PDE9A inhibitor, demonstrating an inhibition concentration (

<p>GNE-618 is a potent and orally active inhibitor of nicotinamide phosphoribosyltransferase (IC50: 6 nM).</p>

<p>ICMT-IN-1 (compound 75) is a potent ICMT inhibitor with an IC50 value of 0.0013 μM.</p>

<p>Tetrahydro-11-dehydrocorticosterone is an inhibitor of 11β-hydroxysteroid dehydrogenase [1].</p>

<p>GLX481304 is a selective Nox-2 and Nox-4 inhibitor, exhibiting IC50 values of 1.25 μM.</p>

<p>4′-DTMP (4-Demethyltrimethoprim) is a DHFR inhibitor with antimicrobial activity against Escherichia coli.</p>

<p>RORγt agonist 2 is a potent agonist of RORγt.</p>

<p>Aladotrilat is an inhibitor of neutral endopeptidase. Its prodrug is aladrotril.</p>

<p>Tiracizine HCl, a new class I antiarrhythmic drug, was studied in patients with ischemic heart disease and shown to decrease myocardial contractile function.</p>

<p>SREBP/SCAP-IN-2 (compound 13) acts as a selective inhibitor of SREBP/SCAP [1].</p>

<p>LMPTP INHIBITOR 1 hydrochloride is a selective inhibitor of low molecular weight protein tyrosine phosphatase ( LMPTP ), with an IC 50 of 0.8 μM for LMPTP-A.</p>

<p>GPX4-IN-2 is a potent inhibitor of GPX4, exhibiting antiproliferative activity. It holds potential for cancer research applications.</p>

<p>ICMT-IN-3 (Compound 27) serves as a potent inhibitor of ICMT, demonstrating an IC50 value of 0.015 μM [1].</p>

<p>Curcumin-β-D-glucuronide, a principal metabolite detected in hepatic tissue and portal blood following oral consumption of Curcumin, is utilized in colon cancer</p>

<p>BMS-962212: reversible, selective FXIa blocker, well-tolerated, quick PD effect, rapid clearance, alters clotting time/activity.</p>

<p>1,2-Diheptadecanoyl-sn-glycero-3-phosphorylcholine (DHPC) is a derivative of phosphatidylcholine (PC) that exhibits biological activity, functioning as a</p>

<p>Quercetin 7-glucuronide (Quercetin 7-O-β-glucuronide), a Quercetin metabolite found in Madagascarian Uncarina species, has the capability to inhibit LDL</p>

<p>SHP2-IN-17 (compound 192) is a potent inhibitor of SHP2, exhibiting an IC50 of 2 nM and holds potential for use in glioblastoma research [1].</p>

<p>ICMT-IN-20 (compound 54) serves as an ICMT inhibitor with an IC50 value of 0.682 μM [1].</p>

<p>RXPA 380: C-terminal ACE inhibitor, Ki=3nM; IC50=2.5nM for C-domain ACE mutants.</p>

<p>PPAR agonist 1 is an agonist of PPAR α/γ, used for reducing blood glucose, lipid levels, reducing body weight, and lowering cholesterol.</p>

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

<p>1,2,3-Tritricosanoyl glycerol, a triacylglycerol containing tricosanoic acid at the sn-1, sn-2, and sn-3 positions, serves as an internal standard for the quantification of fatty acids within the triglyceride component of human aortic endothelial cells (HAECs) cultured in media supplemented with stearic and/or oleic acid.</p>

<p>7,7-Dimethyl-(5Z,8Z)-eicosadienoic acid (DEDA, 5 μM) significantly impacts the response to βA(25-35) stimulation. It reduces the formation of ROS.</p>

<p>ICMT-IN-27, also known as compound 64, is an inhibitor of the enzyme ICMT, demonstrating potent activity with an IC50 value of 0.1 µM [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>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>1,2-Dioleoyl-3-docosohexaenoyl-rac-glycerol, a triacylglycerol, consists of oleic acid at the sn-1 and sn-2 positions and docosahexaenoic acid at the sn-3 position. This compound has been identified in human breast milk.</p>