Metabolism

<p>Cis-13-Octadecenoic acid, a monounsaturated fatty acid, is identified in bovine milk fat.</p>

<p>ATX inhibitor 21 is a potent inhibitor of ATX (IC50: 3490 nM).</p>

<p>Iomazenil is an antagonist and partial inverse agonist of benzodiazepine and potential therapy for alcohol abuse.</p>

<p>2-Myristyldistearin (SMS), a triacylglycerol comprising myristic acid and stearic acid [1], showcases its intricate structural composition.</p>

<p>TID43, a CK2 inhibitor, exhibits potent inhibition with an IC50 value of 0.3 μM. It is applicable in anti-angiogenic research [1].</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>GSK321 is an IDH1 inhibitor that prevents cytoplasmic glutamine reductive carboxylation.GSK321 is used in the study of leukemia.</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>S-Benzylglutathione acts as a competitive inhibitor of glutathionase and undergoes conversion by rat kidney microsomes into its cysteine derivatives.</p>

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

<p>5,6-dehydro Arachidonic acid, an arachidonic acid analog with a 5,6 acetylene, inhibits 5-LO; Ki=15 μM in RBL cells, IC50=10 μM in guinea pig leukocytes.</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>WT IDH1 Inhibitor 2 blocks wild-type and R132H mutant IDH1 (IC50: 120 nM); related to GSK321.</p>

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

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

<p>"(±)-2'-Hydroxy Ceramide (d18:0/18:0) is a sphingomyelin derivative isolated from mammalian platelets upon ADP stimulation [1]."</p>

<p>N-Palmitoyl taurine, an amino-acyl endocannabinoid prominent in rat brain lipidomics profiling, accompanies multiple arachidonoyl amino acids isolated from bovine brain, including N-arachidonoylethanolamine (NADA) and N-arachidonoyl serine (ARA-S). Mass spectral lipidomic analysis of rat brain additionally revealed a series of fatty acyl amides with taurine. The function of N-Palmitoyl taurine is under investigation.</p>

<p>ICMT-IN-37 (compound 41) serves as an inhibitor of ICMT with an IC50 value of 0.308 μM [1].</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>Miglustat hydrochloride (N-Butyldeoxynojirimycin hydrochloride) is an inhibitor of glucosylceramide synthase and can be used for studies about Type I Gaucher</p>

<p>1,2-Dilauroyl-sn-glycero-3-phospho-(2R)-glycerol is a type of phosphoglycerol characterized by the presence of lauric acid at the sn-1 and sn-2 positions. [Matreya, LLC. Catalog No. 1443]</p>

<p>Darodipine (PY-108068) is a dihydropyridine type Ca+2 antagonist.</p>

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

<p>Glycosidase-IN-2 is a glycosidase inhibitor with hypoglycemic activity.</p>

<p>GSK-8062 is an agonist of farnesoid X receptor (FXR).</p>

<p>IDH1 Inhibitor 7 is an IDH1 inhibitor with an IC 50 of less than 100 nM .</p>

<p>ICMT-IN-33 (compound 73) functions as an ICMT inhibitor with an IC50 value of 0.46 μM [1].</p>

<p>SHP2-IN-19 (compound 183) is a SHP2 inhibitor exhibiting potent activity with an IC50 of 3 nM, and is utilized in glioblastoma research [1].</p>

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

<p>MSI-1436 is a selective, non-competitive the enzyme protein-tyrosine phosphatase 1B (PTB1B)inhibitor(IC50 of appr 1 μM)</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>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>

<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>Hemipyocyanine (528-71-2) is the virulence factor of Gram-negative, aerobic rod bacterium Pseudomonas aeruginosa. Hemipyocyanine is an α-Amylase inhibitor.</p>

<p>UK 357903, a phosphodiesterase 5A (PDE5A) inhibitor, is used potentially for the treatment of erectile dysfunction.</p>

<p>5(S)-HETrE, made by 5-LO from mead acid, has unknown biological activity and metabolic fate.</p>

<p>Lp-PLA2-IN-9, a tetracyclic pyrimidinone, inhibits rhLp-PLA2 (pIC50: 10.1), promising for neurodegenerative research.</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>15-PGDH-IN-2 (Compound 2) is an inhibitor of 15-PGDH with an IC50 value of 0.274 nM. This compound is useful for research into hair loss, bone formation, gastric ulcer healing, and dermal wound healing [1].</p>

<p>1-Stearoyl-2-hydroxy-sn-glycero-3-PG, a lysophospholipid characterized by the presence of stearic acid (18:0) at the sn-1 position, finds application in the creation of micelles, liposomes, and various artificial membranes, including those utilized in lipid-based drug delivery systems.</p>

<p>Kelatorphan is an enkephalin degrading enzyme full inhibitor.</p>

<p>(R)-Avanafil ((R)-TA1790) is a selective phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.2 nM, utilized for the research of erectile dysfunction [1</p>

<p>PDE12-IN-3 is an inhibitor of phosphodiesterase 12 (PDE12) (pXC50 of 7.68),with antiviral activity.</p>

<p>DGAT1-IN-1 is a potent inhibitor of diacylglycerol O- acyltransferase type 1(DGAT1, IC50 of &lt; 10 nM).</p>

<p>Efipladib is a phospholipase inhibitor. Efipladib decreases nociceptive responses without affecting PGE2 levels in the cerebral spinal fluid.</p>

<p>Fatty acid amide hydrolase (FAAH), an enzyme responsible for the hydrolysis and inactivation of fatty acid amides like anandamide and oleamide, has been identified as a target by the potent FAAH inhibitor PHOP. PHOP demonstrates remarkable inhibitory activity with K_i values as low as 0.094 nM for human FAAH and 0.2 nM for rat FAAH. Additionally, through a proteomics assay focusing on the serine hydrolase enzyme family, to which FAAH belongs, PHOP's selectivity was evaluated, presenting IC_50 values of 1.1 nM against FAAH, 1.4 nM against triacylglycerol hydrolase (TGH), and greater than 100 µM against an uncharacterized hydrolase (KIAA1363). This specificity profile of PHOP underscores its potential for yielding precise outcomes in studies involving complex biological systems.</p>

<p>RORγt agonist 3 is a potent agonist of RORγt.</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>IDH1 Inhibitor 2 (compound 13) is a potent IDH1 inhibitor via direct covalent modification of His315 (IC50: 110 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>