Metabolismo

<p>(R)-Azasetron besylate (SENS-401), an orally active calcineurin inhibitor, has been shown to mitigate cisplatin-induced hearing loss and cochlear damage [1][2].</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>Cholesterylamine, a cationic lipid, can be incorporated into PLGA to create particles with a charged surface, facilitating its use in drug delivery systems and</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>PPARγ agonist 8, a compound that acts on the peroxisome proliferator-activated receptor gamma (PPARγ), has been shown to stimulate peroxisome proliferator</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>HSD17B13-IN-2 (compound 1) serves as a potent inhibitor of hydroxysteroid 17ß-dehydrogenase 13 (HSD17B13) with demonstrable activity in cellular experiments [1</p>

<p>JGB-1-155, serving as a positive allosteric modulator (N-PAMs), effectively enhances the activity of nicotinamide phosphoribosyltransferase (NAMPT) with an EC 50 of 3.29 μM. It mitigates oxidative stress by elevating NAD+ levels in THP-1 human monocytes and reduces TNFα-induced reactive oxygen species (ROS) in HT-22 cells [1].</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>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>NUCC-0223619 is an IDO1 inhibitor that induces the degradation of IDO protein and can be involved in the synthesis of PROTAC.</p>

<p>ATX inhibitor 15, an indole-based carbamate, has a 2.17 nM IC50 against ATX, suppresses pro-fibrotic genes, and protects against mouse lung fibrosis.</p>

<p>C16 1-Deoxyceramide (m18:1/16:0) is a lipid molecule that can be used in life science related research. The CAS number of C16 1-Deoxyceramide (m18:1/16:0) is 1246298-56-5.</p>

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

1-Deazaadenosine, an adenosine deaminase inhibitor (Ki: 0.66 μM), may treat cancer, particularly lymphoproliferative disorders.

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

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

<p>ICMT-IN-6 (compound 29) serves as an inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), exhibiting an inhibitory concentration 50 (IC50) value of</p>

<p>HSD17B13-IN-3 (compound 2) is a potent inhibitor of hydroxysteroid 17ß-dehydrogenase 13 (HSD17B13), lacking cellular experimental activity [1].</p>

Fasidotril inhibits NEP/ACE, treats high blood pressure in rats, effective in humans with hypertension.

<p>XL041 (BMS-852927) is an agonist of LXRβ-selective.</p>

<p>Lithium benzoate, an aromatic alcohol present in numerous plants, commonly serves as an additive in food, beverages, cosmetics, and various other products. This compound exhibits antibacterial and antifungal properties, functioning effectively as a preservative [1].</p>

<p>Cholesterol 24-hydroxylase-IN-2 is a potent inhibitor of cholesterol 24-hydroxylase (CH24H or CYP46A1), exhibiting an IC50 value of 5.4 nM, and has potential</p>

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

<p>FXIa-IN-1 is a potent β-lactam covalent heparin-derived factor XIa (fXIa) inhibitor.</p>

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

<p>GSK-8062 is an agonist of farnesoid X receptor (FXR).</p>

<p>11-Dehydro Thromboxane B3 (11-dehydro TXB3) serves as a urinary metabolite of TXA3 in humans following an increased dietary intake of EPA.</p>

<p>1,2-Dinonadecanoyl-sn-glycero-3-PC (DNPC), a saturated phospholipid, serves as a standard in quantifying phosphatidylcholines in human synovial fluid and has been utilized in researching lipid bilayer phase transition dynamics.</p>

OSMI-1: cell-permeable OGT inhibitor, blocks O-GlcNAcylation (IC50: 2.7 μM), no effect on other cell glycans.

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

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

<p>PF-04937319 activates glucokinase (EC50=154.4μM) with low hypoglycemia risk, researched for type 2 diabetes treatment.</p>

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

Autotaxin-IN-4 is an Autotaxin inhibitor. It has the potential to treat idiopathic pulmonary fibrosis.

<p>Cyclophellitol aziridine, an analogue of cyclophenol, serves as a potent inhibitor of β-glucosidase [1].</p>

<p>BMS-986318: potent FXR agonist, EC50=53/350 nM, good ADME, effective in liver disease models, for nonalcoholic steatohepatitis research.</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>MK-0736 is a potent and selective 11β-HSD-1 inhibitor.</p>

<p>N-Acyl taurines, such as N-lignoceroyl taurine, alongside various arachidonoyl amino acid conjugates like N-arachidonoyl dopamine and N-arachidonoyl-L-serine, have been identified in bovine brain and through mass spectrometry lipidomic studies in the brain and spinal cord of both wild-type and FAAH knockout mice. Notably, N-lignoceroyl taurine levels were found to be 23-26 times higher in FAAH knockout mice than in wild types, suggesting its degradation by FAAH, despite in vitro evidence showing FAAH hydrolyzes N-lignoceroyl taurine significantly slower than oleoyl ethanolamide. Additionally, N-acyl taurines with polyunsaturated acyl chains are known to activate TRPV1 and TRPV4 channels within the transient receptor potential (TRP) family of calcium channels.</p>

<p>Hypusine is an N-terminal amino alcohol derivative of Lys occurring in bovine brain &amp;</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>Raloxifene Bismethyl Ether hydrochloride is a Raloxifene metabolite and an estrogen receptor inactive compound on which both hydroxyl groups are absent.</p>

<p>GW-6604 is an ALK5 inhibitor and shows clear antifibrotic effects resulting in liver function improvement.</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>YM17E is an inhibitor of ACAT with IC50 of 44 nM in rabbit liver microsomes in vitro.</p>

<p>MLS000545091 is a potent and selective human epithelial 15-lipoxygenase-2 mixed-type inhibitor.</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>9(Z),11(Z)-Octadecadienoic acid, an isomer of linoleic acid, demonstrates antitumor activity with an EC50 value of 446.1 µM [1].</p>