Metabolism

<p>Clopidogrel-β-D-glucuronide is a metabolite of Clopidogrel. It directly interacts with the CYP2C8 enzyme and strongly inhibits the hepatic enzyme CYP2C8.</p>

<p>PDE5-IN-8 (compound 2) is an inhibitor of PDEs.</p>

<p>CYP2C1/CYP2C19-IN-2 is a potent inhibitor of CYP2C9/CYP2C19 without liver toxicity or genotoxicity and can be used to study Zika virus (ZIKV) infection.</p>

<p>β-Glucuronidase/hCAII-IN-2 is a potent inhibitor of β-glucuronidase and hCA II, and their IC50 values were 670.7 μM and 21.77 μM, respectively.</p>

<p>IDX375 is a non-nucleoside inhibitor that selectively targets the HCV NS5B enzyme. It shows promising selectivity for genotypes 1a and 1b. The structure and binding sites of IDX375 have been confirmed through X-ray co-crystallization studies.</p>

<p>(S)-Dexfadrostat ((S)-Fadrozole), an aromatase inhibitor, exhibits an IC 50 of 4.6 nM in in vitro assays using human placental microsomes. It is applicable for research on estrogen-dependent breast cancer, gynecomastia, and systemic lupus erythematosus.</p>

<p>BAY R3401 is an orally active inhibitor of glycogen phosphorylase, leading to irreversible and non-selective inhibition of liver glycogenolysis. It suppresses glycogen breakdown in hepatocytes with IC50 values of 27.06 μM in HL-7702 cells and 52.83 μM in HepG2 cells. BAY R3401 is applicable for research in type 2 diabetes.</p>

<p>Darlifarnib (Compound (S)-058) is an inhibitor of farnesyl transferase and geranylgeranyltransferase, with IC50 values of ≤ 10 nM and &gt; 1000 nM, respectively. It exhibits high metabolic stability in human and mouse liver microsomes, with a half-life of over 100 minutes.</p>

<p>(+)-Potassium Ds-threo-isocitrate monobasic is a bioactive compound known for its role in enhancing cellular metabolism and regulating energy production. This substance is also utilized in researching metabolic pathways and the regulation of enzyme activities. Widely applied in biochemical research, (+)-Potassium Ds-threo-isocitrate monobasic is studied for its potential functions in cellular processes and disease mechanisms.</p>

<p>TAK-915: potent, brain-ready PDE2A inhibitor, 0.61 nM IC50, 4100x selectivity over PDE1A.</p>

<p>Compound 7c inhibits carbonic anhydrase II, lowering intraocular pressure in glaucomatous rabbits.</p>

<p>ATUX-8385 is a potent activator of PP2A. It binds to the PR65 subunit and holds promise for research into cancer and chronic diseases, including Alzheimer's disease and chronic obstructive pulmonary disease (COPD).</p>

<p>RORγt inverse agonist 29 is a potent, selective, orally active RORγt inverse agonist with an IC50 value of 21 nM.</p>

<p>RO5101576 is a potent antagonist of LTB4 receptor.</p>

<p>Carbonic anhydrase inhibitor 9 targets hCA II and IX with Ki of 56.4 and 56.9 nM respectively; shows antiproliferative activity.</p>

<p>CK1δ-IN-10 (Compound 85) is an inhibitor of casein kinase 1 (CK1), specifically targeting CK1δ (CSNKID), with an IC50 value of 0.255 μM.</p>

<p>CA IX-IN-1 (compound 12g) is a potent and highly selective hCA IX inhibitor (IC50: 7 nM) that exhibits antitumour effects.</p>

<p>1-Stearoyl-sn-glycerol 3-phosphate sodium, a biologically active phospholipid, plays a crucial role in regulating cell motility, proliferation, invasion, survival, and the production of growth factors through interactions with G protein-coupled receptors (GPCR). Synthesized during the formation of membrane phospholipids, this compound typically has a low plasma concentration (approximately 100nM) and originates from various cell types, including activated platelets, epithelial cells, leukocytes, neuronal cells, and tumor cells. Its distinctive structure features stearic acid at the sn-1 position and a hydroxyl group at the sn-2 position.</p>

<p>hCA VB-IN-1 (compound 15) is a potent and selective inhibitor of hCA VB (carbonic anhydrase) with a KI of 515.7 nM [1].</p>

<p>Gcase activator 2 is a β-glucocerebrosidase activator that induces dimerization of GCase, increases lysosomal substrate metabolism.</p>