Metabolism

<p>FAS-IN-1 Tosylate is an effective fatty acid synthase inhibitor;Has an IC50 of 10 nM.</p>

<p>3-Hydroxycarbofuran, a principal metabolite of Carbofuran, acts as a reversible inhibitor of acetylcholinesterase (AChE) [1].</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>Frunexian (EP-7041) is a selective and potent inhibitor of coagulation factor XI/activated factor XI, specifically targeting XIa.</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>BMS641 (BMS-209641) is a RARβ agonist with affinity for RARβ that synergistically activates RARβ and RARgamma to induce cell maturation.</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>cis-Clopidogrel-MP derivative, also Clopidogrel-MP-AM, is a 3'-methoxyacetophenone Clopidogrel metabolite and oral P2Y12 receptor platelet inhibitor.</p>

<p>IDH889: Brain-penetrant, mutant-specific IDH1 inhibitor; selective for IDH1 R132* mutations. IC50: 0.02μM (R132H), 0.072μM (R132C), 1.38μM (wild-type).</p>

<p>Eucalyptacid A, a metabolite with antifungal properties, demonstrates efficacy against Alternaria solani, displaying minimum inhibitory concentrations (MIC)</p>

<p>DPM-1001 is an orally bioavailable and non-competitive protein-tyrosine phosphatase (PTP1B) inhibitor (IC50: 100 nM) with the anti-diabetic property.</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>

<p>N-Arachidonoyl dopamine (NADA) and N-Arachidonoyl serine (ARA-S), among various arachidonoyl amino acids, have been extracted from bovine brain, while a novel series of fatty acyl amides of taurine were unearthed in rat brain through mass spectral lipidomic analysis, indicating the discovery of a new class of compounds also located in the kidney. These compounds are known to activate members of the transient receptor potential (TRP) family of calcium channels. Notably, N-Stearoyl taurine emerges as a significant amino-acyl endocannabinoid identified in rat brain lipidomics profiling.</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>Arbaprostil, a synthetic PGE analog, guards stomach lining, aids ulcer healing, and blocks pancreatic function and tumor growth.</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>ICMT-IN-39, also known as compound 18, functions as an inhibitor of ICMT with an IC50 value of 0.031 µM [1].</p>

<p>Lp-PLA2-IN-2 is a selective and potent lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 0f 120 nM for recombinant human Lp-PLA2.</p>

<p>(S)-(-)-Bay-K-8644 ((S)-(-)-Bay K 8644) is an agonist of L-type Ca2+ channel and activates Ba2+ currents with an EC50 of 32 nM.</p>

<p>(R)-tert-OMe-byakangelicin, a furanocoumarin, exhibits inhibitory effects on liver drug metabolizing enzyme (DME) activity and can be isolated from the immature</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>ICMT-IN-50 (compound 3) serves as an inhibitor of ICMT with an IC50 value of 0.31 µM [1].</p>

<p>C2 Dihydro Ceramide (d18:0/2:0) (C2 Dihydroceramide) is a ceramide that is a precursor of ceramide synthesis and stimulates ABCA1-mediated cholesterol efflux.</p>

<p>D-threo-PDMP inhibits glucoceramide synthase, cutting cell surface glycosphingolipids and hindering neurite growth.</p>

<p>4-Methylumbelliferyl-α-D-Glucopyranoside (4MU-αGlc) is a fluorescence substrate for α-glucosidase, serving as a biomarker for Fabry disease and Pompe disease</p>

<p>Tisolagiline (KDS2010) is a potent, highly selective and reversible MAO-B inhibitor oral activity for the treatment of Alzheimer's disease and obesity.</p>

<p>FASN-in-1 is an effective, specific inhibitor of fatty acid synthase (FASN), a compound specifically designed to target and inhibit the activity of the enzyme</p>

<p>1-Palmitoyl-2-lauroyl-sn-glycero-3-PC (1,2-PLPC) is a phospholipid with palmitoyl (16:0) and lauryl (12:0) acyl chains at the sn-1 and sn-2 positions, respectively. This mixed-chain phosphatidylcholine aids in researching the role of chain-chain contact interactions in maintaining the structural stability of lipid membrane bilayers.</p>

<p>MγLnFP, an analog of methyl arachidonyl fluozophosphonate (MAFP), holds significance in pharmacological research due to its potential as an inhibitor of phospholipases, FAAH, and its role as a CB receptor ligand. However, the properties and effects of the γ-linolenyl variant of MAFP remain to be fully explored.</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>Glycolithocholic acid (Lithocholic acid glycine conjugate) is a glycine conjugate of lithocholic acid.</p>

<p>Zopolrestat (CP 73850) is a potent inhibitor of aldose reductase (IC50 = 3.1 nM).</p>

<p>GSK3987 is an LXR ligand. GSK3987 recruits the steroid receptor coactivator-1 to human LXRalpha and LXRbeta with EC50s of 40 nM.</p>

<p>Lateritin (Bassiatin) is An Acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor and a platelet aggregation inhibitor from the mycelial cake of Gibberella</p>

<p>PHD2-IN-1, a potent and orally active HIF prolyl hydroxylase 2 (PHD2) inhibitor, exhibits an IC50 of 22.53 nM and is applicable in anemia research [1].</p>

<p>RORγt inverse agonist 14 (8e) is a potent, selective, and orally active compound with an EC50 of 2.5 nM, exhibiting anti-inflammatory activity.</p>

<p>VULM 1457 is a potent ACAT inhibitor.</p>

<p>Bemoradan is an inhibitor of the rolipram-insensitive cyclic AMP phosphodiesterase from canine heart tissue</p>

<p>ICMT-IN-47 (compound 26) acts as an ICMT inhibitor with an IC50 value of 0.76 μM [1].</p>

<p>L-869298 is a potent and selective inhibitor of PDE4.</p>

<p>15-deoxy-Δ12,14-Prostaglandin D2 (15-deoxy-Δ12,14-PGD2) is a PGD2 metabolite functioning as an agonist for the PGD2 receptor 2 (DP2), with a binding affinity (Ki) of 50 nM for the mouse DP2 receptor expressed in HEK293 cell membranes. It activates eosinophils with an EC50 of 8 nM and enhances the recruitment of steroid receptor coactivator-1 (SRC-1) to peroxisome proliferator-activated receptor γ (PPARγ), initiating PPARγ-mediated transcription at 5 µM concentration. Furthermore, it exhibits cytotoxicity towards L1210 murine leukemia cells with an IC50 of 0.3 µg/ml and displays weaker inhibition of ADP-induced platelet aggregation than PGD2, with an IC50 of 320 ng/ml.</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>ICMT-IN-53 (compound 12) is an ICMT inhibitor exhibiting an IC50 of 0.96 μM, alongside favorable PAMPA permeability and antiproliferative properties.</p>

<p>Niraxostat (Y-700) is one of the isocytosine derivatives as xanthine oxidase inhibitors.</p>

<p>Metformin hydroxy analog 2, an oxidation product of the biguanide metformin (1), represents a chemically transformed variant of the original compound, showcasing a modified molecular structure through the process of oxidation.</p>

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

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

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