Métabolisme

1-Deazaadenosine, an adenosine deaminase inhibitor (Ki: 0.66 μM), may treat cancer, particularly lymphoproliferative disorders.

HSD17B13-IN-3 (compound 2) is a potent inhibitor of hydroxysteroid 17ß-dehydrogenase 13 (HSD17B13), lacking cellular experimental activity [1].

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

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

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

Quizalofop (Xylafop) is a reagent of biochemical.

ICMT-IN-9 (compound 47) is a potent ICMT inhibitor with an IC50 value of 0.16 μM [1].

MMV009085 is a potent inhibitor of the Plasmodium falciparum hexose transporter (Pf HT1), with potential as an anti-malarial agent.

FTI-2153 inhibits farnesyltransferase with 1.4 nM IC50, >3000x more effective on H-Ras than Rap1A.

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

Dioleyldimethylammonium chloride (DODAC) is a cationic lipid utilized as a transfection reagent [1].

Monohydroxy melphalan, a degradation product and DNA alkylating agent derived from melphalan, results from melphalan hydrolysis in aqueous solutions such as cell culture medium and human plasma. It enhances DNA adducts in ML-1 myeloblastic leukemia cells based on concentration and induces cytotoxicity with an IC50 value of 28.1 μg/ml.

ATX-001, an ionizable cationic lipid, is utilized in the creation of lipid nanoparticles (LNPs) for mRNA delivery [1].

TMP780 is an inverse RORγt agonist (IC50: 13 nM). RORγt is a tractable drug target for the treatment of cutaneous inflammatory disorders.

AKB-6899 is an inhibitor of prolyl hydroxylase domain 3 (PHD3) and increases the soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated

Safinamide acid, a potential impurity in commercial safinamide preparations and a degradation product of safinamide under thermal and oxidative stress, is encountered in the pharmaceutical formulation process.

CKD-519: A CETP inhibitor with an IC50 of 2.3 nM, blocking cholesteryl ester transfer in serum.

IDO1/2-IN-1 hydrochloride: Dual IDO1/2 inhibitor, IC50 of 28/144 nM, oral, with antitumor properties.

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.

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.