Métabolisme

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

FR-186054, a potent ACAT inhibitor with high oral efficacy, outperforms others in vitro regardless of dosage.

<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>DNCA, a neutral lipid, facilitates the creation of lipid nanoparticles (LNPs) and is instrumental in [nucleic acid delivery](1).</p>

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

<p>MK-0736 is a potent and selective 11β-HSD-1 inhibitor.</p>

<p>Aladotrilat is an inhibitor of neutral endopeptidase. Its prodrug is aladrotril.</p>

secreted phospholipase A2 (sPLA2) inhibitor

<p>Tiracizine HCl, a new class I antiarrhythmic drug, was studied in patients with ischemic heart disease and shown to decrease myocardial contractile function.</p>

<p>FXIa-IN-7 is an orally available, selective and potent inhibitor of factor XIa for the study of thrombophilia.</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>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>AGN 193109 is a potent antagonist of retinoic acid receptors (RARs; Kd= 2, 2, and 3 nM for RARα, β, and γ, respectively), exhibiting selectivity for RARs over retinoid X receptors (RXRs; Kd= &gt;10,000 nM for human RXRα, β, and γ receptors). This compound effectively reverses cellular morphology changes and growth suppression induced by RAR agonists such as all-trans-RA, 13-cis-RA, and 9-cis-RA in ECE16-1 human endometrial ectocervical epithelial cells, particularly when used at a 10-fold molar excess. Furthermore, AGN 193109 downregulates the expression of cytokeratin K5-8, 13, 14, 16, 17, and 19 genes, indicating inhibition of retinoid action, specifically when co-administered with TTNPB but not as a standalone treatment. In vivo studies demonstrate teratogenic effects, including cleft palate, frontonasal dysplasia, and eye malformations in mouse fetuses following a single oral dose of 1 mg/kg.</p>

<p>MLS000545091 is a potent and selective human epithelial 15-lipoxygenase-2 mixed-type inhibitor.</p>

<p>SHP2-IN-18 (compound 183) is a potent SHP2 inhibitor, exhibiting an IC50 of 3 nM and applicable to glioblastoma research [1].</p>

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

<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>

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>EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM. EMD638683 R-Form is the R-form of EMD638683.</p>

<p>sEH/AChE-IN-4-15 is a dual sEH and AChE inhibitor crossing the BBB, with IC50s: 3.1 nM (hsEH), 1660 nM (hAChE), 179 nM (hBChE), 14.5 nM (msEH), 102 nM (mAChE).</p>

<p>LNK754 is a farnesyltransferase inhibitor. It is used for the treatment of cancer and Alzheimer's disease.</p>

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

5-Lipoxygenase-In-1 (compound example 4.10) is a 5-Lipoxygenase inhibitor.

<p>Mutant IDH1-IN-4 is an mutant Isocitrate dehydrogenase 1 (IDH 1) inhibitor.</p>

<p>A 78773: potent reversible 5-lipoxygenase inhibitor; active in cells/tissues; targets inflammation, asthma, IBD.</p>

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

<p>S-Benzylglutathione acts as a competitive inhibitor of glutathionase and undergoes conversion by rat kidney microsomes into its cysteine derivatives.</p>

<p>1,3-Dipalmitoyl glycero-2-phosphatidylethanolamine is a phospholipid incorporating saturated long-chain (16:0) stearic acid at the sn-1 and sn-3 positions, with phosphatidylethanolamine (PE) at the sn-2 position. Phosphatidylethanolamines, critical components of biological membranes, play essential structural and functional roles. Various PE types are instrumental in forming micelles, liposomes, and other synthetic membranes.</p>

<p>ERX-41 is an orally active, stereospecific small molecule that targets lysosomal acid lipase A (LIPA).</p>

<p>ICMT-IN-50 (compound 3) serves as an inhibitor of ICMT with an IC50 value of 0.31 µM [1].</p>

<p>PDP-EA is an activator of fatty acid amide hydrolase(FAAH) and enhances the amidohydrolase activity of FAAH.</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>WT IDH1 Inhibitor 2 blocks wild-type and R132H mutant IDH1 (IC50: 120 nM); related to GSK321.</p>

<p>GNE-6468 is a potent and selective agonist of RORγ(RORc) (EC50: 13 nM for HEK-293 cell).</p>

<p>Compound 22g: potent GLO1 inhibitor; IC50=0.011 μM; potential for depression, anxiety research.</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>S-2E, an oral inhibitor of HMG-CoA reductase/acetyl-CoA carboxylase, treats hyperlipidemia.</p>

<p>MetAP2-IN-1 is a selective inhibitor of MetAP2, a target involved in angiogenesis-related conditions, suitable for research applications [1].</p>

<p>Leukotriene C4 (14,15-LTC4) is an inflammatory mediator synthesized from arachidonic acid through the actions of 15- and 12-lipoxygenases (LOs), involving intermediates such as 15-HpETE and 14,15-LTA4. Unlike the majority of leukotrienes formed via the 5-LO pathway, 14,15-LTC4 is an eoxin predominantly produced by eosinophils, although mast cells and nasal polyps can also synthesize it. While its physiological roles are not well understood, 14,15-LTC4 exhibits limited contractile activity on guinea pig ileum and pulmonary parenchyma. However, it can increase vascular permeability in human endothelial cell monolayers in vitro with potency comparable to 5-LO-derived leukotrienes, contributing to plasma leakage characteristic of inflammation.</p>

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

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

<p>Lp-PLA2-IN-9, a tetracyclic pyrimidinone, inhibits rhLp-PLA2 (pIC50: 10.1), promising for neurodegenerative research.</p>

<p>YG1702, a potent inhibitor specific to ALDH18A1, suppresses the proliferation of MYCN-amplified neuroblastoma (NB) and reduces MYCN expression.</p>

<p>17(S)-HpDHA, primarily produced by the 15-Lipoxygenase (LOX) isoenzymes h15-LOX-1 and h15-LOX-2 from docosahexaenoic acid (DHA), is a key regulator in epoxide synthesis through allosteric modulation. Additionally, it effectively inhibits platelet aggregation, demonstrating an EC50 of approximately 1 μM [1].</p>

<p>FR-190809 is a nonadrenotoxic and orally efficacious inhibitor of acyl-CoA:cholesterol O-acyltransferase (ACAT) (IC50: 45 nM).</p>

<p>Sampatrilat, an oral vasopeptidase inhibitor, more potently blocks C-domain ACE (Ki=13.8 nM) over N-domain (Ki=171.9 nM).</p>

<p>ICMT-IN-54 (compound 7c), an adamantyl analogue, serves as an ICMT inhibitor with an IC50 value of 12.4 μM, targeting the methylation process facilitated by</p>

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

<p>QH536 degrades HMGCR (EC50: 0.22 μM), has anti-inflammatory properties, and avoids cholesterol buildup; useful for cardiovascular and NASH research.</p>

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

<p>BMS-962212: reversible, selective FXIa blocker, well-tolerated, quick PD effect, rapid clearance, alters clotting time/activity.</p>

<p>Homonojirimycin is an alpha-glucosidase inhibitor.</p>

<p>ICMT-IN-26 (compound 38) acts as an ICMT inhibitor with an IC50 value of 0.36 μM [1].</p>

<p>LY-338979 is an impurity of pemetrexedone.</p>

<p>Arachidonoyl amide (AMC-AA) is a fatty acid amide among several that serve to quantify fatty acid amide hydrolase (FAAH) activity. FAAH, with its relative lack of selectivity, processes various amide head groups beyond ethanolamine, the head group of its primary endogenous substrate, anandamide (AEA). The interaction of AMC-AA with FAAH leads to the liberation of fluorescent aminomethyl coumarin, which has an absorption peak at 360 nm and emission at 465 nm. This fluorescence release facilitates the rapid and efficient assessment of FAAH activity through the utilization of either a standard cuvette or a microplate fluorometer.</p>

<p>Ilepatril, also known as AVE-7688, is a vasopeptidase inhibitor for the treatment of hypertension.</p>

<p>9(E),11(E)-Conjugated Linoleic Acid (9(E),11(E)-CLA) belongs to a group of eight geometric isomers of linoleic acid, characterized by adjacent double bonds. This specific isomer, 9,11 all-trans linoleic acid, was first discovered in ground beef and is found in various dairy products as well. Notably, it has been shown to decrease mammary tumors in rats with dietary inclusion as minimal as 0.1%. [Matreya, LLC. Catalog No. 1181]</p>

PF-04957325 is an inhibitor of PDE8.PF-04957325 has an IC50 of 0.7 nM for PDE8A.PF-04957325 can be used for the study of autoimmune encephalomyelitis.

<p>2-Myristyl dipalmitin (PMP), a triglyceride of palmitic acid, shows potential as a lipid marker for Wilson's disease (WD) [1] [2].</p>

<p>11-Hexadecenoic acid, a monounsaturated fatty acid, comprises both 11-cis-hexadecenoic acid and 11-trans-hexadecenoic acid. These isoforms are present in ewe milk fat and their concentrations increase when the diet is supplemented with lipids from linseed, sunflower, olive, or fish oils. Additionally, 11-trans-hexadecenoic acid is found in intramuscular fat of both male and female foals. The product is a blend of the 11-cis and 11-trans forms. [Matreya, LLC. Catalog No. 1208]</p>

<p>G1-OC2-K3-E10, an ionizable lipid, facilitates mRNA delivery through lipid nanoparticles (LNPs) [1].</p>

<p>ICMT-IN-13 (compound 49) functions as an inhibitor of ICMT, exhibiting an IC50 value of 0.47 μM [1].</p>

<p>CETP-IN-3 is an inhibitor of the plasma glycoprotein cholesterol ester transfer protein (CETP), elevating HDL-C through inhibition of CETP.</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>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>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>Lp-PLA2-IN-13 (compound 15), a potent Lp-PLA2 inhibitor, holds potential for research in neurodegenerative-related diseases [1].</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>Mal-Pc, a maleimide phthalocyanine, depletes GSH to reduce aggregation and boost ROS, improving PDT against cancer.</p>

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

<p>h-NTPDase-IN-5 (compound 3b) serves as a pan-inhibitor of NTPDase, exhibiting inhibitory concentration 50 (IC50) values of 1.10 μM (h-NTPDase1), 44.73 μM (h-</p>

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

<p>Taurohyocholic acid (THCA), a taurine-conjugated form of porcine-specific primary bile acid hyocholic acid, inhibits cholesterol crystal precipitation by stabilizing cholesterol in the liquid-crystalline phase and prevents cholestasis and cellular necrosis in isolated rat livers induced by taurolithocholic acid. Additionally, THCA levels rise in the urine of patients with hepatitis B-induced cirrhosis.</p>

<p>Oxalomalic acid (Oxalomalate) trisodium, an inhibitor of aconitase and NADP-dependent isocitrate dehydrogenase, suppresses nitrite production and inducible nitric oxide synthase (iNOS) protein expression in lipopolysaccharide-activated J774 macrophages [1].</p>

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

<p>SCD1/5-IN-1 (Compound 10), a selective SCD1/5 inhibitor, is utilized in the research of neurological diseases [1].</p>

<p>H2-003 is a selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2).</p>

FM26, an isoxazole-based RORγt inverse agonist, cuts EL4 IL-17a mRNA; potent with 264 nM IC50.

Inz-1 is an effective and fungal-selective inhibitor of mitochondrial cytochrome bc1 with IC50s of 8.092 and 45.320 μM for yeast and human.

<p>BMS-986318: potent FXR agonist, EC50=53/350 nM, good ADME, effective in liver disease models, for nonalcoholic steatohepatitis research.</p>

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

<p>Benzyl-α-GalNAc (O-glycosylation-IN-1) is a potent inhibitor of O-glycosylation and is used to reduce mucin on cell surfaces.</p>

<p>BBT has anti-hyperglycemic activity, protecting beta cells from cytokine or streptozotocin-induced cell death, and restoring beta cell function.</p>

<p>TMDJ-035 is a selective inhibitor of the RyR2 (ryanodine receptor 2).</p>

<p>ICMT-IN-44 (compound 23) serves as an ICMT inhibitor with an IC50 value of 0.167 μM [1].</p>

<p>12(R)-HEPE, a monohydroxy fatty acid derived from EPA in the eggs of the sea urchin S. purpuratus, has a biological activity that, while not extensively documented, may resemble that of 12(R)-HETE (Catalog No.34560).</p>

<p>ICMT-IN-32 (compound 70) acts as an inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), demonstrating an IC50 value of 0.777 µM [1].</p>

<p>JTT 551: Selective PTP1B inhibitor for type 2 diabetes research; Ki=0.22μM for PTP1B, 9.3μM for TCPTP.</p>

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

<p>RORγt Inverse agonist 3 is a potent, selective and orally active inverse agonist of RORγ(EC50s of 0.22 μM and 0.15 μM for hRORγ and RORγt (human IL-17 cells),</p>

A 62198 is a potent and selective renin inhibitor with potential as a hypotensive agent.

<p>SMS1-IN-1 is a potent inhibitor of sphingomyelin synthase 1 (SMS1, IC50 = 2.1 μM), and can be used in the atherosclerosis studies.</p>

<p>DSTAP chloride (CDESA), a cationic lipid, is utilized in the formation of lipid nanoparticles (LNPs) and exhibits high transfection efficiency [1].</p>

<p>Compound 1e, also known as ALP/Carbonic anhydrase-IN-1, is a dual inhibitor targeting both carbonic anhydrase (CA) isozymes II, IX, and XII, as well as alkaline</p>

<p>C16 1-Deoxyceramide (m18:1/16:0) is a lipid molecule that can be used in life science related research. The CAS number of C16 1-Deoxyceramide (m18:1/16:0) is 1246298-56-5.</p>

<p>1-Myristoyl-2-linoleoyl-3-oleoyl-rac-glycerol, a triacylglycerol, features myristic acid, linoleic acid, and oleic acid at the sn-1, sn-2, and sn-3 positions, respectively. This compound is prevalent in mature human milk, infant formula fats, and butterfat.</p>

<p>C22 Phytoceramide (t18:0/22:0) is a lipid molecule that can be used in life science related research. The CAS number of C22 Phytoceramide (t18:0/22:0) is 164576-03-8.</p>

<p>SREBP/SCAP-IN-2 (compound 13) acts as a selective inhibitor of SREBP/SCAP [1].</p>