Metabolism

<p>Cav 3.2 Inhibitor 4 (Compound 21) is a selective and potent inhibitor of the T-type calcium channel (Ca v 3.2), demonstrating peripheral restriction with an</p>

<p>1,2-Dilinoleoyl-sn-glycero-3-PC (Dilinoleoyllecithin), a phospholipid, finds application in the production of artificial membranes [1].</p>

<p>S-(p-Nitrobenzyl)glutathione acts as a competitive inhibitor of glutathionase.</p>

<p>BMS-185411 is a bio-active chemical.</p>

<p>Chinese gallotannin, a non-specific promiscuous inhibitor of α-amylase, exhibits a K(i) value of 0.82 μg/mL against human salivary α-amylase and shows potential</p>

<p>DOG-IM4 is a chemical compound instrumental in synthesizing nanoparticles for delivering antigen-encoding nucleic acids, targeting a broad range of conditions including autoimmune diseases, rare blood or metabolic disorders, allergies, cancer, and infectious diseases [1].</p>

<p>1-Oleoyl-2-hydroxy-sn-glycero-3-PG (sodium salt), a lysophospholipid with oleic acid (18:1) at the sn-1 position, finds application in creating micelles, liposomes, and various artificial membranes, notably in lipid-based drug delivery systems.</p>

<p>Yonkenafil, a PDE5 inhibitor, may reduce stroke damage and aid in Alzheimer's treatment.</p>

<p>CJ-463, a selective uPA blocker, shows strong anti-tumor effect, especially at 100mg/kg, potentially treating lung cancer.</p>

<p>Desacetyl bisacodyl, the active metabolite of the laxative bisacodyl, evokes epithelial Cl(-) secretion in the rat colon and rectum, in addition to increasing</p>

<p>AS 183 is an inhibitor of cholesterol acyltransferase (ACAT).</p>

<p>8(Z),14(Z)-Eicosadienoic Acid, an ω-8 C20:2 fatty acid, constitutes 0.19% of total fatty acids in human milk. In vivo, it is converted by desaturases into eicosatrienoic acids, known for their potent vasodilator properties. However, the physiological effects of 8(Z),14(Z)-Eicosadienoic Acid remain unexplored.</p>

<p>DLPA is a phosphatidic acid (PA) that incorporates the medium-chain lauric acid (12:0).</p>

<p>KRP-109, a neutrophil elastase (NE) inhibitor, acts by decreasing expression of TGF-ß Signal Related Genes.</p>

<p>15-PGDH-IN-1: potent oral 15-PGDH inhibitor, IC50=3nM, useful for tissue repair research.</p>

<p>PDE1-IN-2 is an PDE1 inhibitor(PDE1C, PDE1B and PDE1A with IC50 values of 6, 140 and 164 nM, respectvely).</p>

<p>A 79175 is a 5-lipoxygenase inhibitor that increases bone formation.</p>

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

<p>KH064 is a sPLA2-IIA inhibitor of oral activity.</p>

<p>hCAIX-IN-15 is a potent inhibitor of human carbonic anhydrase IX (hCA IX) with an inhibition constant (Ki) of 38.8 nM, exhibiting broad-spectrum anticancer</p>

<p>α-Glucosidase-IN-28 (Compound 18) is an α-glucosidase inhibitor with an IC50 of 0.62 μM and Ki value of 3.93 μM.</p>

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

<p>Compound 144 (also known as Anticancer Agent 144) is a potent inhibitor of both PTPN2 and PTP1B, exhibiting IC50 values of less than 2.5 nM, making it suitable</p>

<p>Sulforhodamine 101 DHPE, a fluorescent probe, results from the conjugation of sulforhodamine 101, a red fluorescent dye with excitation/emission spectra of 586/605 nm, to the phospholipid 1,2-dipalmitoyl-sn-glycero-3-PE. It effectively integrates into phospholipid bilayers and is utilized for imaging solid supported lipid bilayers, detecting protein-ligand interactions on bilayers, and monitoring lipid probe colocalization in liposomes through resonance energy transfer (RET).</p>

<p>hCAIX/XII-IN-8 (compound 3g) is a potent inhibitor of the human carbonic anhydrases (CAs) IX and XII, with inhibition constants (K i) of 8.5 nM for CA IX and 6.</p>

<p>FTI-276 is an inhibitor of protein farnesyltransferase (PFT) (IC50s: 0.9 and 0.5 nM for Plasmodium falciparum and human).</p>

<p>1,2-Dimyristoyl-3-palmitoyl-rac-glycerol (MMP) is a triacylglycerol comprising myristic acid and palmitic acid [1].</p>

<p>Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are a class of endogenous lipids whose levels are modulated by fasting and high-fat diets and are linked to insulin sensitivity. These compounds typically consist of a C-16 or C-18 fatty acid, such as palmitoleic, palmitic, oleic, or stearic acid, esterified to a hydroxylated C-16 or C-18 lipid. One specific form of FAHFA, known as 9-OAHSA, involves the esterification of oleic acid to 9-hydroxy stearic acid. Within the FAHFA family, OAHSAs notably represent the predominant form found in the serum of glucose-tolerant AG4OX mice, which uniquely overexpress the Glut4 glucose transporter in adipose tissue.</p>

<p>PF-915275 inhibits 11βHSD1 in humans (Ki=2.3 nM, EC50=15 nM) and affects cortisone-cortisol conversion in hepatocytes.</p>

<p>L-hydroxylysine dihydrochloride , is formed by posttranslational hydroxylation of some lysine residues. It is an amino acid, is exclusive to collagen protein.</p>

<p>13-OAHSA, a branched fatty acid ester of hydroxy fatty acids (FAHFAs), results from the esterification of oleic acid to 13-hydroxy stearic acid. It represents a significant component of the FAHFA family, most abundantly expressed in the serum of glucose-tolerant AG4OX mice that exhibit adipose tissue-specific overexpression of the Glut4 glucose transporter. Similar to other FAHFAs which are known to enhance glucose tolerance, stimulate insulin secretion, and exert anti-inflammatory effects, 13-OAHSA may play a pivotal role in managing metabolic syndrome and inflammation.</p>

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

<p>3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid) (Dehydrolithocholic acid) is a bile acid metabolite and inhibits the differentiation of TH17 cells by directly</p>

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

<p>Z-Pro-Pro-CHO acts as a prolyl oligopeptidase inhibitor with half-maximal inhibitory concentrations (IC50) of 0.16 μM for human prolyl oligopeptidase and 0.01</p>

<p>Ac-VDVAD-CHO is an inhibitor of caspase-2 and caspase-3 (IC50: 46 nM for caspase-2 and 15 nM for caspase-3) [1].</p>

GSK2973980A is a selective Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) inhibitor (IC50: 3 nM).

<p>PPARδ agonist 9 (compound 21), with an EC50 of 3.6 nM, is effective in vivo, decreasing serum MCP-1 concentrations in mice and markedly reducing atherosclerotic</p>

<p>Gisadenafil besylate (UK 369003-26) is a potent and orally active PDE5 inhibitor, for lower urinary tract symptoms associated with benign prostatic hyperplasia.</p>

<p>GSK2324 is a potent FXR agonist for the treatment of NAFLD by controlling hepatic lipids through reduced uptake and selective reduction of fatty acid synthesis.</p>

<p>Imiglitazar (TAK559) is a potent PPAR-β/δ receptor agonist with hypoglycemic effects.</p>

<p>AZD-1656 is a glucokinase activator (GKA) that can cause dose-limiting hypoglycemia in normal animals used in embryofetal development studies and type 2</p>

<p>RORγt Inverse agonist 6 is an agonist of RORγt inverse. RORγt Inverse agonist 6 can be used in research on Th17-driven autoimmune diseases.</p>

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

<p>NOX2-IN-2 (compound 33) is a potent inhibitor of NOX2, disrupting the p47phox-p22phox protein-protein interaction with a dissociation constant (K i) of 0.24 μM.</p>

<p>Perindopril acyl-β-D-glucuronide is a metabolite of the ACE inhibitor perindopril [1].</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>

hCAIX-IN-16 (Compound 12d), an inhibitor of hCA IX, exhibits inhibition constants (K i) of 190.0 nM for hCA IX and 187.9 nM for hCA XII.

<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>VU0364739, a selective phospholipase D2 (PLD2) inhibitor with an IC50 of 22 nM, effectively reduces cancer cell proliferation [1].</p>