Metabolismo

<p>ICMT-IN-19 (compound 53) serves as a potent inhibitor of ICMT, demonstrating an IC50 value of 0.026 μM [1].</p>

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

<p>QH536 degrades HMGCR (EC50: 0.22 μM), has anti-inflammatory properties, and avoids cholesterol buildup; useful for cardiovascular and NASH research.</p>

<p>DORI, a cationic lipid, efficiently delivers plasmid DNA in vitro, exhibiting lower cytotoxicity and high transfection efficiency [1].</p>

<p>ICMT-IN-46 (compound 25) is a potent inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), exhibiting an IC50 value of 0.556 μM [1].</p>

<p>WT IDH1 Inhibitor 2 blocks wild-type and R132H mutant IDH1 (IC50: 120 nM); related to GSK321.</p>

<p>Tetramyristoylcardiolipin (TMCL), an anionic lipid, plays a crucial role in studying cell membrane function and drug delivery mechanisms [1].</p>

<p>E-5324 is potent cholesterol acyltransferase (ACAT) inhibitor (IC50s: 44 to 190 nM).</p>

<p>BMS-654457 is a small-molecule, reversible inhibitor of factor XIa (FXIa; Kis: 0.2 and 0.42 nM for human and rabbit FXIa).</p>

<p>Arachidonoyl amide (AMC-AA) is a fatty acid amide among several that serve to quantify fatty acid amide hydrolase (FAAH) activity. FAAH, with its relative lack of selectivity, processes various amide head groups beyond ethanolamine, the head group of its primary endogenous substrate, anandamide (AEA). The interaction of AMC-AA with FAAH leads to the liberation of fluorescent aminomethyl coumarin, which has an absorption peak at 360 nm and emission at 465 nm. This fluorescence release facilitates the rapid and efficient assessment of FAAH activity through the utilization of either a standard cuvette or a microplate fluorometer.</p>

<p>LY-338979 is an impurity of pemetrexedone.</p>

<p>FR-190809 is a nonadrenotoxic and orally efficacious inhibitor of acyl-CoA:cholesterol O-acyltransferase (ACAT) (IC50: 45 nM).</p>

<p>Prostaglandin F2α-1-glyceryl ester undergoes oxidation via 15-hydroxyprostaglandin dehydrogenase (15-HPGDH) [1].</p>

<p>Lp-PLA2-IN-14 (Compound 19), an inhibitor of rhLp-PLA2, exhibits a potent inhibitory effect with a pIC50 value of 8.4.</p>

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

<p>Clocortolone pivalate, a synthetic steroid, treats dermatitis and psoriasis.</p>

<p>YG1702, a potent inhibitor specific to ALDH18A1, suppresses the proliferation of MYCN-amplified neuroblastoma (NB) and reduces MYCN expression.</p>

<p>Bucolome (Paramidine) is a CYP2C9 inhibitor with uricosuric and anti-inflammatory activity.</p>

<p>LNK754 is a farnesyltransferase inhibitor. It is used for the treatment of cancer and Alzheimer's disease.</p>

<p>S-Benzylglutathione acts as a competitive inhibitor of glutathionase and undergoes conversion by rat kidney microsomes into its cysteine derivatives.</p>

<p>"Oral FXR antagonist 1 selectively blocks intestinal FXR, with IC50 of 2.1 μM, aiding in NASH research by improving liver health."</p>

<p>II-B08 is a cell-permeable SHP2 inhibitor (IC50 = 5.5 µM). II-B08 blocks growth factor stimulated ERK1/2 activation and hematopoietic progenitor proliferation.</p>

<p>12(R)-HEPE, a monohydroxy fatty acid derived from EPA in the eggs of the sea urchin S. purpuratus, has a biological activity that, while not extensively documented, may resemble that of 12(R)-HETE (Catalog No.34560).</p>

<p>GNE-6468 is a potent and selective agonist of RORγ(RORc) (EC50: 13 nM for HEK-293 cell).</p>

<p>SH-BC-893: Oral anti-cancer sphingolipid analog, prevents ceramide-related mitochondrial issues, and tackles diet-related obesity.</p>

<p>1a,1b-Dihomo Prostaglandin F2α (1a,1b-dihomo PGF2α), a hypothetical product of adrenic acid in the COX pathway, is predominantly synthesized in the renal medulla, reflecting the selective distribution of adrenic acid in this region.</p>

<p>Darodipine (PY-108068) is a dihydropyridine type Ca+2 antagonist.</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>PPACK: synthetic peptide, irreversibly inhibits thrombin (Ki = 0.24 nM), prevents platelet activation.</p>

<p>Entacapone acid (AG 1290) is a selective and reversible inhibitor of catechol-O-methyltransferase(COMT).</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>GW-6604 is an ALK5 inhibitor and shows clear antifibrotic effects resulting in liver function improvement.</p>

<p>113-O16B, an ionizable cationic lipidoid featuring a disulfide bond, is utilized in producing lipid nanoparticles (LNPs) for mRNA delivery [1].</p>

<p>CJ-463, a selective uPA blocker, shows strong anti-tumor effect, especially at 100mg/kg, potentially treating lung cancer.</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>MS-444 (BE-34776) is an MLCK and HuR inhibitor with antitumor activity that can be used to study triple-negative breast cancer and colorectal cancer.</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>(Rac)-Lonafarnib is a racemic FTase inhibitor, effective against H-ras, K-ras, N-ras (IC50: 1.9, 5.2, 2.8 nM), and has anti-HDV properties.</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>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>

<p>1-Palmitoyl-2-oleoyl-sn-glycero-3-PA (1,2-POPA) is a phospholipid featuring a palmitic acid (16:0) chain that is saturated and an oleic acid (18:1) chain that is monounsaturated, positioned at the sn-1 and sn-2 locations, respectively. This compound is utilized in creating micelles, liposomes, and various artificial membrane forms.</p>

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

<p>Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are endogenous lipids that are influenced by fasting and high-fat diets and linked to improved insulin sensitivity in mice. These compounds typically feature a chain of either 16 or 18 carbon atoms (for example, palmitoleic, palmitic, oleic, or stearic acid) esterified with a hydroxy fatty acid chain of similar length. One specific FAHFA, known as 5-OAHSA, consists of oleic acid bonded to the fifth carbon of hydroxy stearic acid. Within the FAHFA family, OAHSAs exhibit the highest serum levels in AG4OX mice, which are known for their glucose tolerance attributed to the overexpression of the Glut4 glucose transporter in adipose tissue.</p>

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

<p>1-Palmitoyl-3-stearoyl-rac-glycerol, a diacylglycerol, features palmitic acid at the sn-1 position and stearic acid at the sn-3 position. This compound appears in palm-based diacylglycerols derived from palm stearin, palm mid fraction, palm oil, and palm olein, as well as in extracts of wheat bran and brewer's spent grain.</p>

<p>Diethyl-pythiDC is an collagen prolyl 4-hydroxylase inhibitor.</p>

TMP780 is an inverse RORγt agonist (IC50: 13 nM). RORγt is a tractable drug target for the treatment of cutaneous inflammatory disorders.

<p>13,14-Dihydro-15(R)-Prostaglandin E1 (13,14-dihydro-15(R)-PGE1) is an analog of 13,14-dihydro-PGE1 characterized by its R-configured hydroxyl group at the C-15 position [1].</p>

<p>1,2-Dioleoyl-3-stearoyl-rac-glycerol, a triacylglycerol, features oleic acid at the sn-1 and sn-2 positions and stearic acid at the sn-3 position. This compound is present in sunflower, corn, and soybean oils, as well as in ostrich oil.</p>

<p>γ-CEHC, a metabolite of γ-tocopherol, is predominantly excreted through urine, primarily in its conjugated form as glucuronide [1], rather than through bile.</p>