Métabolisme

<p>6β-hydroxy Testosterone （4-Androsten-6β,17β-diol-3-one） is a 17β-hydroxy steroid, an androgen and endogenous metabolite.</p>

<p>(R)-Palmitoyl-(2-methyl)ethanolamide (Me-PEA) acts as a competitive inhibitor against [3H]-AEA metabolism, exhibiting a K i value of 6.6 μM [1].</p>

<p>Adibendan (Adibendanum) is a selective inhibitor of PDE3 with an IC50 of 2.0 μM.</p>

<p>SHP2-IN-20 (compound 193), a potent SHP2 inhibitor, exhibits an IC50 of 3 nM, making it suitable for glioblastoma research [1].</p>

<p>RORγt agonist 2 is a potent agonist of RORγt.</p>

<p>SREBP/SCAP-IN-2 (compound 13) acts as a selective inhibitor of SREBP/SCAP [1].</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>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>ICMT-IN-3 (Compound 27) serves as a potent inhibitor of ICMT, demonstrating an IC50 value of 0.015 μM [1].</p>

PTP1B-IN-20: Selective PTP1B inhibitor, IC50=1.05μM; less effective on TCPTP (IC50=78μM), targets type 2 diabetes.

<p>Branched fatty acid esters of hydroxy fatty acids (FAHFAs) have emerged as significant regulators of metabolic processes, influenced by dietary changes such as fasting and high-fat diets, and are linked to improved insulin sensitivity in mice. These compounds typically feature a fatty acid chain, either C-16 or C-18 in length (for example, palmitoleic, palmitic, oleic, or stearic acid), esterified to a hydroxy fatty acid of similar length. A specific FAHFA, 12-POHSA, involves the esterification of palmitoleic acid to the 12th carbon of stearic acid. Notably, 12-POHSA levels are markedly higher in the serum of AG4OX mice, which exhibit enhanced glucose tolerance due to overexpression of the Glut4 glucose transporter in adipose tissue. Given the capacity of FAHFAs to enhance glucose tolerance, stimulate insulin secretion, and exert anti-inflammatory actions, 12-POHSA holds potential as a bioactive lipid implicated in managing metabolic syndrome and inflammation.</p>

<p>C24:1 1-Deoxyceramide (m18:1/24:1(15Z)) is a lipid molecule that can be used in life science related research. The CAS number of C24:1 1-Deoxyceramide (m18:1/24:1(15Z)) is 1246298-58-7.</p>

<p>1-Palmitoyl-2-oleoyl-3-stearoyl-rac-glycerol, a primary triacylglycerol in cocoa butter, features palmitic acid (at the sn-1 position), oleic acid (at the sn-2 position), and stearic acid (at the sn-3 position).</p>

<p>FAAH Inhibitor 2 (Compound 17b) is an irreversible inhibitor of fatty acid amide hydrolase (FAAH), demonstrating an IC50 value of 0.153 μM [1].</p>

<p>SM-32504 is a potent inhibitor of ACAT.</p>

<p>CHK-336 (Example 1), an orally active LDHA inhibitor (IC50 &lt;1 nM), suppresses lactate production in mouse hepatocytes and is applicable in hyperoxaluria</p>

<p>Brodimoprim is an inhibitor of dihydrofolate reductase(DHFR).</p>

<p>Quizalofop-P, a selective herbicide, is absorbed by weed stems and leaves before translocating both upward and downward within the plant, concentrating in</p>

<p>MGAT2-IN-2 is a potent inhibitor of acyl CoA:monoacylglycerol acyltransferase 2 (MGAT2) (IC50 of 3.4 nM).</p>

<p>ICMT-IN-18 (compound 35) serves as an ICMT inhibitor with an IC50 value of 0.066 μM [1].</p>

<p>1,2-Dilauroyl-sn-glycero-3-phosphoethanolamine (DLPE), a phosphatidylethanolamine derivative featuring lauric acid (12:0) acyl chains, serves in the development of liposomes [1].</p>

<p>3-Decyl-5,5'-diphenyl-2-thioxo-4-imidazolidinone (compound 45), having a pI50 of 5.89, shows promise as an inhibitor of fatty acid amide hydrolase (FAAH). Despite its activity, it demonstrates a lack of affinity for cannabinoid receptors CB(1) and CB(2) [1].</p>

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

<p>(±)16,17-EDT, an oxylipin metabolite of adrenic acid produced through the cytochrome P450 (CYP) pathway, effectively induces dilation in isolated porcine</p>

<p>PHD-IN-2 (Compound 91), a potent PHD antagonist with an IC50 of less than 5 nM, effectively stimulates erythropoietin synthesis in HEP3B cells with an EC50 of</p>

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

<p>3-Aminoisobutyric acid, a non-protein amino acid resultant from thymine catabolism, plays a significant role in metabolic activities. At a 5 µM concentration, it triggers browning in primary adipocytes, notably elevating uncoupling protein 1 (UCP-1) and CIDEA expression. Additionally, it boosts PPARα expression in both primary adipocytes and mouse inguinal white adipose tissue (WAT) in vivo, alongside enhancing β-oxidation in hepatocytes. Its plasma levels surge post-exercise in mice, and its administration at 100 mg/kg daily curtails weight gain and body fat without diminishing food consumption or hiking energy output, whilst ameliorating glucose tolerance. Notably, 3-aminoisobutyric acid concentrations are heightened in individuals with β-ureidopropionase deficiency, a genetic flaw impairing pyrimidine degradation, affecting plasma, urine, and cerebrospinal fluid.</p>

<p>M5N36: selective Cdc25C inhibitor, IC50: 0.15µM A, 0.19µM B, 0.06µM C; halts cell growth, boosts p-CDK1/2.</p>

<p>GLUT4 activator 1 is a potent glucose transporter type 4 (GLUT4) translocation activator (EC50: 0.14 μM).</p>

<p>Diflumidone sodium is a non-steroidal agent with anti-inflammatory activity.</p>

<p>Glycolithocholic acid (Lithocholic acid glycine conjugate) is a glycine conjugate of lithocholic acid.</p>

<p>N-Methyl Palbociclib is an impurity of the orally active selective CDK4 and CDK6 inhibitor Palbociclib (PD 0332991).</p>

<p>4′-DTMP (4-Demethyltrimethoprim) is a DHFR inhibitor with antimicrobial activity against Escherichia coli.</p>

<p>AS1468240 is a factor Xa inhibitor. It has significant oral anticoagulant activity.</p>

<p>JNJ-42259152 is a phosphodiesterase 10A PET tracer.</p>

<p>Me-Indoxam is an inhibitor of sPLA2. It has no effect on arachidonic acid release and platelet activating factor synthesis.</p>

<p>CAY10435, a β-ketooxazapyridine and selective FAAH inhibitor, exhibits antimicrobial properties. It binds non-competitively to the FAAH of Dictyostelium discoideum, demonstrating a Kd value of 0.57 nM [1] [2].</p>

<p>Biliverdin, produced through the oxidation of bilirubin, can also be synthesized through a non-protoporphyrin pathway in Corynebacterium glutamicum [1].</p>

<p>ICMT-IN-21 (compound 6ag) is an ICMT inhibitor with an IC50 value of 8.8 µM, featuring sulfonamide-modified farnesyl cysteine (SMFC).</p>

<p>Sch59498 is a potent phosphodiesterase 1c (Pde1c) inhibitor.</p>

<p>Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are lipids that are modulated by dietary changes such as fasting and high-fat diets, and they play a role in insulin sensitivity. These compounds generally consist of a fatty acid chain of either 16 or 18 carbons (for example, palmitoleic, palmitic, oleic, or stearic acid) esterified to a similarly long hydroxy fatty acid. One specific FAHFA, 9-SAHSA, features stearic acid esterified at the 9th carbon of hydroxy stearic acid. The concentration of 9-SAHSA is notably increased in the serum of glucose-tolerant AG4OX mice, which specifically express the Glut4 glucose-transporting protein in adipose tissue.</p>

<p>MAGL-IN-6, a powerful MAGL blocker, IC50 at 4.71 nM, may assist in neurological disease research.</p>

<p>H-0104 Dihydrochloride is an inhibitor of ROCK that acts by applying potent intraocular pressure (IOP)-lowering effects into the eyes of monkeys.</p>

<p>OSMI-2 is a cell-permeable inhibitor of O-linked N-acetylglucosamine transferase (OGT).</p>

<p>BMS-262084 is a potent selective β-lactam trypsin inhibitor with therapeutic potential in the treatment of asthma.</p>

<p>ICMT-IN-1 (compound 75) is a potent ICMT inhibitor with an IC50 value of 0.0013 μM.</p>

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

<p>Gentisuric acid, an Aspirin metabolite and a substrate of α-amidating monooxygenase (PAM), mitigates DNA damage induced by Mitomycin C. [1] [2]</p>

<p>Pactimibe is a ACAT inhibitor. It has anti-atherosclerotic activity.</p>

<p>JGB-1-155, serving as a positive allosteric modulator (N-PAMs), effectively enhances the activity of nicotinamide phosphoribosyltransferase (NAMPT) with an EC 50 of 3.29 μM. It mitigates oxidative stress by elevating NAD+ levels in THP-1 human monocytes and reduces TNFα-induced reactive oxygen species (ROS) in HT-22 cells [1].</p>

<p>9(Z),11(E),13(Z)-Octadecatrienoic acid methyl ester, an isomer of 9(Z),11(E),13(E)-octadecatrienoic acid methyl ester and the methyl ester derivative of 9(Z),11(E),13(Z)-octadecatrienoic acid, serves as a standard for quantifying 9(Z),11(E),13(Z)-octadecatrienoic acid in wild growing pomegranate (P. granatum) seed oil [Matreya, LLC. Catalog No. 1240].</p>

<p>Tetrahydro-11-dehydrocorticosterone is an inhibitor of 11β-hydroxysteroid dehydrogenase [1].</p>

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

<p>GLX481304 is a selective Nox-2 and Nox-4 inhibitor, exhibiting IC50 values of 1.25 μM.</p>

<p>First potent oral dual IDO1/IDO2 inhibitor with antitumor properties; IC50: 28 nM (IDO1), 144 nM (IDO2).</p>

<p>S-2E, an oral inhibitor of HMG-CoA reductase/acetyl-CoA carboxylase, treats hyperlipidemia.</p>

<p>GSK2256294A (GSK 2256294) is potent, selective inhibitor of recombinant human, rat and mouse sEH with IC50 of 27 pM, 61 pM and 189 pM, respectively.</p>

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

<p>1,2-Distearoyl-3-oleoyl-rac-glycerol, a triacylglycerol, comprises stearic acid at the sn-1 and sn-2 positions and oleic acid at the sn-3 position. This compound is present in cocoa butter and vegetable oils.</p>

<p>Temocaprilat (RS5139) is an Angiotensin-converting Enzyme (ACE) inhibitor.</p>

<p>VU0155069 hydrochloride (CAY10593 hydrochloride) is a potent and selective inhibitor of phospholipase D (PLD), exhibiting IC50 values of 46 nM for PLD1 and 933 nM for PLD2. It effectively inhibits the migration of both human and mouse breast cancer cell lines [1] [2].</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>L-690488 has more effective cell penetration than L-690330. L-690488 is a prodrug of L-690330 and is a selective inositol monophosphatase (IMPase) inhibitor.</p>

<p>CL4H6, a pH-sensitive cationic lipid, serves as the primary constituent of lipid nanoparticles (LNPs). These LNPs are instrumental in targeting and delivering siRNA, leading to a potent gene-silencing response [1] [2].</p>

<p>CYP3A4-IN-2, a potent CYP3A4 inhibitor (IC50: 0.055 μM), is a hydrophobic ritonavir analog with immunosuppressive and antiviral properties.</p>

<p>"9322-O16B, an ionizable cationic lipid, facilitates the generation of lipid nanoparticles (LNPs) [1]."</p>

<p>GNE-618 is a potent and orally active inhibitor of nicotinamide phosphoribosyltransferase (IC50: 6 nM).</p>

<p>C12-113, a lipidoid delivery agent, effectively transfects siRNA into cells and, when combined with additional lipids, forms lipid nanoparticles (LNPs). These LNPs facilitate the delivery of mRNA encoding the spike glycoprotein of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in mice [1] [2].</p>

<p>DMPA, a derivative of phosphatidic acid (PA), constitutes a significant component of cellular membranes.</p>

<p>LB-60-OF61 is a NAMPT inhibitor, a NAMPT inhibitor that displays antiproliferative activity against MYC oncogene-dependent cancer cell lines.</p>

<p>Ionizable Lipid-2 (Compound 1) serves as an ionizable lipid, essential for nucleic acid delivery and the construction of lipid nanoparticles (LNPs) [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>

Quizalofop (Xylafop) is a reagent of biochemical.

<p>ICMT-IN-43 (compound 22) acts as a potent inhibitor of the enzyme ICMT, exhibiting an inhibitory concentration (IC50) value of 0.04 μM [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>ICMT-IN-6 (compound 29) serves as an inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), exhibiting an inhibitory concentration 50 (IC50) value of</p>

<p>5-OP-RU is a MAIT-activating ligand, a major antigen of MAIT cells, a mucosal adjuvant, and can be used to study Mycobacterium tuberculosis infection.</p>

<p>ICMT-IN-38 (Compound 42) is an ICMT inhibitor, demonstrating an IC50 value of 0.049 μM [1].</p>

<p>Prostaglandin F2α-1-glyceryl ester undergoes oxidation via 15-hydroxyprostaglandin dehydrogenase (15-HPGDH) [1].</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>ICMT-IN-51 (compound 43) serves as an ICMT inhibitor with an IC50 value of 0.55 μM [1].</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>Diethyl-pythiDC is an collagen prolyl 4-hydroxylase inhibitor.</p>

<p>VT-1598 tosylate is a selective, orally active antifungal compound that targets CYP51. It demonstrates efficacy against C. auris.</p>

<p>H-0106 Dihydrochloride is an inhibitor of ROCK that acts by applying strong intraocular pressure (IOP)-lowering effects into the eyes of monkeys.</p>

EMT inhibitor-2 blocks CYP3A4 and CYP2C9 (IC50: 49.72, 5.54 μM) and prevents IL-1β/TGF-β-induced EMT.

<p>L791943 is a selective, potent) inhibitor of Phosphodiesterase-4 (PDE4,IC50 of 4.2 nM).</p>

<p>RB 101 suppresses enkephalinase and aminopeptidases; biologically cleaved at disulfide to produce inhibitors of both aminopeptidase N and neutral endopeptidase.</p>

<p>ICMT-IN-25 (compound 37) serves as a potent inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), exhibiting an IC50 value of 0.025 μM [1].</p>

<p>HIF-2α-IN-9 (compound 35r) serves as an HIF-2α inhibitor, effectively suppressing VEGF-A with an IC50 of 305 nM, and modulating growth-promoting genes within</p>

<p>Lp-PLA2-IN-13 (compound 15), a potent Lp-PLA2 inhibitor, holds potential for research in neurodegenerative-related diseases [1].</p>

<p>JP104 is an aryl carbamate that irreversibly inhibits fatty acid amide hydrolase (FAAH) with a pIC50 value of approximately 8 [1].</p>

<p>Mal-Pc, a maleimide phthalocyanine, depletes GSH to reduce aggregation and boost ROS, improving PDT against cancer.</p>

<p>CA Inhibitor 12 strongly blocks CA II (K_i 1.72 nM), also inhibits CA I (271 nM), shows anticancer effects.</p>

<p>GPX4-IN-4 (Compound 24) serves as a potent inhibitor of GPX4, applicable in cancer research [1].</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>IDH1 Inhibitor 2 (compound 13) is a potent IDH1 inhibitor via direct covalent modification of His315 (IC50: 110 nM).</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>

OSMI-1: cell-permeable OGT inhibitor, blocks O-GlcNAcylation (IC50: 2.7 μM), no effect on other cell glycans.

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