Metabolismo

<p>11-Dehydro-2,3-Dinor Thromboxane B2 is a metabolite of Thromboxane B2 (TXB2), formed by the oxidation of TXB2 via 11-Hydroxy Thromboxane Dehydrogenase.</p>

<p>Enpp-1-IN-4: potent enpp-1 inhibitor with potential in cancer research. See patent WO2019177971A1, compound 1.</p>

<p>Homonojirimycin is an alpha-glucosidase inhibitor.</p>

<p>ICMT-IN-13 (compound 49) functions as an inhibitor of ICMT, exhibiting an IC50 value of 0.47 μM [1].</p>

<p>AZD 4017 is an inhibitor of 11β-Hydroxysteroid Dehydrogenase Type 1(11β-HSD1) (IC50: 7 nM).</p>

<p>244cis, an ionizable cationic lipid incorporating a piperazine structure, facilitates the creation of lipid nanoparticles (LNPs). These LNPs, when formulated with 244cis and coated with an mRNA reporter gene, exhibit preferential accumulation in the lungs of mice, in contrast to those formulated with SM-102. Additionally, it leads to a reduction in the levels of serum chemokine (C-C motif) ligand 2 (CCL2) [1].</p>

<p>Lignoceroyl ethanolamide, a fatty N-acyl ethanolamine within the endocannabinoid family, is derived from lignoceric acid, which is found in relatively high concentrations in rat cerebrospinal fluid. However, the specific function and significance of this metabolite remain unclear.</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>HIF-2α-IN-13 (18) acts as a HIF-2α inhibitor and exhibits an IC 50 value of 2.7 μM.</p>

<p>Darglitazone (CP-86325) is a potent, selective agonist of PPAR-γ with antidiabetic actions.</p>

<p>Palmitoleic acid, an ω-7 monounsaturated fatty acid found in macadamia and sea buckthorn oils, enhances both basal and insulin-stimulated glucose uptake, as well as Glut4 protein levels in 3T3-L1 adipocytes at a 200 µM concentration. Ex vivo, at a dosage of 300 mg/kg per day, it significantly increases glucose uptake and both aerobic and anaerobic glycolysis, while decreasing de novo fatty acid synthesis and the activity of lipogenic enzymes, specifically ATP citrate lyase (ACL) and glucose-6-phosphate dehydrogenase (G6PDH), in isolated murine adipocytes. Furthermore, the dietary administration of palmitoleic acid at 300 mg/kg mitigates high-fat diet-induced insulin resistance and liver inflammation in mice.</p>

<p>Monoacylglycerol lipase inhibitor 1, also known as compound 13 [1], is a potent inhibitor of monoacylglycerol lipase.</p>

<p>GGTI-2133: potent GGTase I inhibitor, IC50=38 nM; blocks inflammatory cell invasion in mice asthma.</p>

<p>PDE7-IN-3 (Example 2) serves as an inhibitor of phosphodiesterase PDE7 and exhibits potential analgesic properties.</p>

<p>ZK824859 is an oral uPA inhibitor with IC50s: 79 nM (uPA), 1580 nM (tPA), 1330 nM (plasmin).</p>

<p>9(Z),11(E)-Conjugated Linoleic Acid Methyl Ester, identified in lemon grass (C. flexuosus), serves as a standard for quantifying conjugated linoleic acids in thermally stressed olive oil and trans fats in bakery products. [Matreya, LLC. Catalog No. 1255]</p>

<p>JW 618 is a selective inhibitor of ABHD6, demonstrating inhibition concentrations (IC50 values) of 38 nM for mouse ABHD6 and 13 nM for rat ABHD6, indicating its potent activity across species [1].</p>

<p>Thioquinapiperifil is a type of phosphodiesterase-5 (PDE-5) inhibitor found in dietary supplements.</p>

<p>ICMT-IN-9 (compound 47) is a potent ICMT inhibitor with an IC50 value of 0.16 μM [1].</p>

<p>FTI-2153 inhibits farnesyltransferase with 1.4 nM IC50, &gt;3000x more effective on H-Ras than Rap1A.</p>