Metabolismo

<p>ICMT-IN-32 (compound 70) acts as an inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), demonstrating an IC50 value of 0.777 µM [1].</p>

<p>ICMT-IN-41 (compound 20) serves as a potent inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), demonstrating an IC50 value of 0.069 μM [1].</p>

<p>RORγt Inverse agonist 3 is a potent, selective and orally active inverse agonist of RORγ(EC50s of 0.22 μM and 0.15 μM for hRORγ and RORγt (human IL-17 cells),</p>

<p>Bemfivastatin hemicalcium (PPD 10558), an orally active HMG-CoA reductase inhibitor, serves as a lipid-lowering agent.</p>

<p>AS1468240 is a factor Xa inhibitor. It has significant oral anticoagulant activity.</p>

<p>5-PAHSA, a FAHFA formed through the formal condensation of the carboxy group of palmitic acid with the hydroxy group of 5-hydroxystearic acid, serves as a human metabolite, possesses anti-inflammatory and hypoglycemic properties, and is categorized as a long-chain fatty acid. This compound, deriving from hexadecanoic acid and octadecanoic acid, is the conjugate acid of a 5-PAHSA(1-).</p>

<p>IDH1 Inhibitor 2 (compound 13) is a potent IDH1 inhibitor via direct covalent modification of His315 (IC50: 110 nM).</p>

<p>1,2-Dilauroyl-sn-glycero-3-phosphoethanolamine (DLPE), a phosphatidylethanolamine derivative featuring lauric acid (12:0) acyl chains, serves in the development of liposomes [1].</p>

<p>3-Decyl-5,5'-diphenyl-2-thioxo-4-imidazolidinone (compound 45), having a pI50 of 5.89, shows promise as an inhibitor of fatty acid amide hydrolase (FAAH). Despite its activity, it demonstrates a lack of affinity for cannabinoid receptors CB(1) and CB(2) [1].</p>

<p>(±)16,17-EDT, an oxylipin metabolite of adrenic acid produced through the cytochrome P450 (CYP) pathway, effectively induces dilation in isolated porcine</p>

<p>3-Aminoisobutyric acid, a non-protein amino acid resultant from thymine catabolism, plays a significant role in metabolic activities. At a 5 µM concentration, it triggers browning in primary adipocytes, notably elevating uncoupling protein 1 (UCP-1) and CIDEA expression. Additionally, it boosts PPARα expression in both primary adipocytes and mouse inguinal white adipose tissue (WAT) in vivo, alongside enhancing β-oxidation in hepatocytes. Its plasma levels surge post-exercise in mice, and its administration at 100 mg/kg daily curtails weight gain and body fat without diminishing food consumption or hiking energy output, whilst ameliorating glucose tolerance. Notably, 3-aminoisobutyric acid concentrations are heightened in individuals with β-ureidopropionase deficiency, a genetic flaw impairing pyrimidine degradation, affecting plasma, urine, and cerebrospinal fluid.</p>

<p>α-Glucosidase-IN-29 (compound 19) is an inhibitor of α-glucosidases, exhibiting an IC50 value of 1.21 μM and a Ki of 1.80 μM.</p>

<p>CYP17-IN-1 is an effective oral inhibitor of CYP17 that can inhibit CYP17 in rats and humans with IC50 of 15.8 and 20.1 nM.</p>

<p>SREBP/SCAP-IN-1 (compound 10b) serves as a selective inhibitor of SREBP/SCAP [1].</p>

<p>Pactimibe sulfate is a dual ACAT1/2 inhibitor with anti-atherogenic potential, reducing plasma cholesterol.</p>

<p>C24:1 dihydro 1-Deoxyceramide (m18:0/24:1) is a lipid molecule that can be used in life science related research. The CAS number of C24:1 dihydro 1-Deoxyceramide (m18:0/24:1) is 1246298-60-1.</p>

<p>8(Z)-Eicosenoic acid, a cis-unsaturated free fatty acid featuring a 20-carbon chain, enhances acetylcholine (ACh) receptor channel currents without causing depression and augments PCKε phosphorylation of a substrate peptide in Xenopus oocytes. This acid comprises 6% of the fatty acid composition in seed oil extracted from B. collina.</p>

<p>9(E),11(E)-Conjugated Linoleic Acid (9(E),11(E)-CLA) belongs to a group of eight geometric isomers of linoleic acid, characterized by adjacent double bonds. This specific isomer, 9,11 all-trans linoleic acid, was first discovered in ground beef and is found in various dairy products as well. Notably, it has been shown to decrease mammary tumors in rats with dietary inclusion as minimal as 0.1%. [Matreya, LLC. Catalog No. 1181]</p>

<p>Pactimibe is a ACAT inhibitor. It has anti-atherosclerotic activity.</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>