Métabolisme

ICMT-IN-17 (compound 52) serves as an ICMT inhibitor, exhibiting an IC50 value of 0.38 μM [1].

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

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.

Adomeglivant (LY2409021) is a potent glucagon receptor blocker, reducing blood glucose in type 2 diabetes with minimal side effects.

5(S)-HETE lactone is an ester inhibiting rat leukemia cell 5-lipoxygenase (IC50=27μM), potentially due only to the 5(S) form; untested enantiomers.

ICMT-IN-34 (compound 39) serves as an effective inhibitor of ICMT, exhibiting an IC50 value of 0.17 μM [1].

IDH1 Inhibitor 5 targets MOG cells (IC50: 64.4 nM) and R132H mutant IDH1 gliomas (IC50: 34.9 nM).

1,2-Dioleoyl-3-α-linolenoyl-rac-glycerol, a triacylglycerol, features oleic acid at the sn-1 and sn-2 positions and α-linolenic acid at the sn-3 position. This compound has been identified in the fat body of male B. lapidarius bumblebees.

cKK-E15, a peptide-lipid, is instrumental in formulating LNP3 alongside C14PEG2000, unmodified cholesterol, and DOPE [1].

GSK2647544 inhibits Lp-PLA2, a pro-inflammatory enzyme from macrophages, orally active, calcium-independent.

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).

14,15-Epoxyeicosatrienoic acid (14,15-EET), derived from Arachidonic acid metabolism, significantly inhibits platelet aggregation in vivo and enhances

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.

XR3054 is a farnesyl protein transferase inhibitor that blocks proliferation in certain cancer cells, not dependent on ras mutation status.

1-Palmitoyl-sn-glycerol 3-phosphate (1-P-GPA), an endogenous metabolite, is utilized in the research of non-alcoholic fatty liver disease [1].

1,2-Dipalmitoyl-sn-glycero-3-N,N-dimethyl-PE is a derivative of 1,2-dipalmitoyl-sn-glycero-3-PE (1,2-DPPE) with two added methyl groups on its sn-3 moiety, which in aqueous suspensions, reduces the phase transition temperature relative to those of 1,2-DPPE and 1,2-dipalmitoyl-sn-glycero-3-N-methyl-PE (1,2-NMeDPPE). It is utilized in creating liposomes and monolayers for investigating membrane permeability and monolayer viscosity.

Lansoprazole N-oxide is a potential impurity in lansoprazole bulk preparations, identified as a degradation product under acidic or basic conditions. This compound is related to lansoprazole, a proton pump inhibitor.

ICMT-IN-12 (compound 78) serves as an ICMT inhibitor, demonstrating an IC50 value of 0.42 μM [1].

COX-2-IN-30, a benzenesulfonamide derivative, is an orally active, dual inhibitor of cyclooxygenase-2 (COX-2; IC50 = 49 nM) and cyclooxygenase-1 (COX-1; IC50 =

Windaus ketone functions as a vitamin D (VD) synthesis inhibitor.

11(Z)-Docosenoic acid, a 22-carbon monounsaturated fatty acid, is identified in fish oil.

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

(Rac)-Lonafarnib is a racemic FTase inhibitor, effective against H-ras, K-ras, N-ras (IC50: 1.9, 5.2, 2.8 nM), and has anti-HDV properties.

4-epiMinocycline, recognized as a primary degradation product and a probable impurity in minocycline commercial formulations, is derived from minocycline, a broad-spectrum tetracycline antibiotic notable for its extended serum half-life. Besides treating acne, especially in older patients, minocylvania exhibits significant anti-inflammatory and neuroprotective effects.

FXa-IN-1, an FXa blocker: IC50=3 nM, Ki=0.7 nM, orally available, long half-life, for thrombosis research.

IDH1 Inhibitor 2 (compound 13) is a potent IDH1 inhibitor via direct covalent modification of His315 (IC50: 110 nM).

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

RP 70676 is a potent ACAT inhibitor(rat and rabbit ACAT with IC50 of 25 and 44 nM ).

17(R)-Resolvin D3 (17(R)-RvD3) is an aspirin-triggered epimer of resolvin D3, produced from docosahexaenoic acid (DHA) through the action of COX-2 in the presence of aspirin, via a 17(R)-hydroperoxy DHA (17(R)-HDHA) intermediary. Identified in mouse inflammatory exudates, 17(R)-RvD3 notably inhibits the transmigration of isolated human polymorphonuclear cells (PMNs) and fosters the efferocytosis of apoptotic PMNs by macrophages. Furthermore, in a mouse model of zymosan-induced peritonitis, 17(R)-RvD3 administration (10 ng/animal) significantly curtails neutrophil infiltration into the peritoneal cavity and modulates cytokine levels by reducing IL-6 and increasing IL-10 in the inflammatory exudate. It engages GPR32, evidenced by activation in a β-arrestin reporter assay and augments phagocytosis more effectively in CHO cells overexpressing GPR32 compared to controls. Additionally, 17(R)-RvD3 enhances the clearance of etoposide-induced tumor cell debris by monocyte-derived macrophages in H460 human lung carcinoma.

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.

BMS-654457 is a small-molecule, reversible inhibitor of factor XIa (FXIa; Kis: 0.2 and 0.42 nM for human and rabbit FXIa).

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.

Clocortolone pivalate, a synthetic steroid, treats dermatitis and psoriasis.

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

CI-1044 is an inhibitor of PDE4 (IC50s: 0.29, 0.08, 0.56, 0.09 μM for PDE4A5, PDE4B2, PDE4C2 and PDE4D3).

N-Desethyl-N-methyl Vardenafil, a potential impurity in commercial vardenafil preparations, functions as a phosphodiesterase 5 (PDE5) inhibitor, similar to its parent compound. With an IC50 value of 2 nM, it exhibits potent inhibitory activity against PDE5.

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

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

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

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

NC1 is a potent allosteric inhibitor of lymphoid-specific PTPN22, a protein tyrosine phosphatase.

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

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

Prostaglandin H2 (PGH2), initially isolated from the incubation of arachidonic acid with ovine seminal vesicle microsomes, acts as a potent vasoconstrictor. It serves as the precursor for all 2-series prostaglandins (PGs) and thromboxanes (TXs). Moreover, as a TP receptor agonist, PGH2 irreversibly aggregates human platelets at concentrations of 50-100 ng/ml.

LMPTP INHIBITOR 1 hydrochloride is a selective inhibitor of low molecular weight protein tyrosine phosphatase ( LMPTP ), with an IC 50 of 0.8 μM for LMPTP-A.

1,2-Dioleoyl-3-docosohexaenoyl-rac-glycerol, a triacylglycerol, consists of oleic acid at the sn-1 and sn-2 positions and docosahexaenoic acid at the sn-3 position. This compound has been identified in human breast milk.

Quetiapine sulfoxide dihydrochloride, a major metabolite of second-gen antipsychotic Quetiapine, modulates 5-HT and dopamine receptors.

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.

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

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