fabp

BMS309403 is a potent and selective inhibitor of adipocyte fatty acid binding protein aFABP. It improves endothelial function in apolipoprotein E-deficient mice and cultured human endothelial cells. It interacts with the fatty acid binding pocket inside the protein and competitively inhibits the binding of endogenous fatty acids.

FABP-IN-2, a novel ligand for FABP3, demonstrates inhibition of both FABP3 and FABP4 with IC50 values of 1.16 μM and 4.27 μM, respectively.

FABPs ligand 6 (MF6) is a selective inhibitor of FABP5 and FABP7 that reduces levels of oxidative stress in the mouse spinal cord as well as lipopolysaccharide-stimulated interleukin-1β and tumor necrosis factor α accumulation in primary astrocyte cultures.FABPs ligand 6 has a potent protective function in oligodendrocytes of EAE mice through FABP5 inhibition. mitochondria with a strong protective function.

FABP4-IN-2 (Compd 10g), a selective and orally active FABP4 inhibitor, exhibits K i values of 0.51 μM for FABP4 and 33.01 μM for FABP3, demonstrating its specificity towards FABP4. It is utilized in research investigating inflammatory diseases [1].

FABP4 5-IN-4 (compound E1) effectively inhibits FABP 4 and FABP 5, displaying IC50 values of 3.78 μM and 5.72 μM, respectively. It is significant in the management of metabolic disorders such as diabetes mellitus [1].

FABP4 5-IN-5 (compound D9) serves as a potent inhibitor of both FABP 4 and FABP 5, demonstrating IC50 values of 4.68 μM and 10.72 μM, respectively. It is notably effective in addressing metabolic disorders such as diabetes mellitus [1].

FABP4-IN-4 (Compound 30) is an orally effective inhibitor of FABP, with an IC50 value of 1.18 μM against FABP1. In a mouse model of diet-induced obesity, FABP4-IN-4 improves glucose tolerance, reduces levels of blood sugar, lipids, and liver inflammation markers, alleviates hepatic steatosis, and exhibits anti-inflammatory activity.

STK-15 is a candidate for use as an inhibitor of fatty acid binding protein 5 (FABP5).

ABP/PPAR modulator 1 is an orally active multi-regulator of FABP and PPAR, exhibiting IC50 values of 0.65 μM for FABP1 and 1.08 μM for FABP4, and EC50 values of 9.19 μM, 2.20 μM, and 1.58 μM for PPARα, PPARγ, and PPARδ, respectively. It demonstrates potent activity against metabolic dysfunction-associated steatohepatitis (MASH). Additionally, ABP/PPAR modulator 1 dose-dependently improves various pathological features of fatty liver in a WD + Carbon tetrachloride-induced MASH mouse model.

HTS01037 is a fatty acid-binding inhibitor and a competitive antagonist of protein-protein interactions mediated by AFABP aP2 (Ki: 0.67 μM).

HM-50316 is a High affinity FABP4 inhibitor (Ki < 1 nM).

BMS-309403 sodium is a potent, orally active, selective inhibitor of adipocyte fatty acid binding protein (FABP4, aP2), with inhibitory constants (Ki) of <2 nM for FABP4, 250 nM for FABP3, and 350 nM for FABP5. It competitively binds to the fatty-acid-binding pocket of the protein, impeding the attachment of endogenous fatty acids. This compound enhances endothelial function in apolipoprotein E-deficient mice and cultured human endothelial cells, underlining its potential therapeutic benefits [1] [2] [3].

CooP, a linear glioblastoma-targeting nonapeptide, interacts with the mammary-derived growth inhibitor fatty acid binding protein 3 (FABP3) found in glioblastoma cells and their associated blood vessels. This interaction facilitates the targeted delivery of chemotherapy and various nanoparticles [1].

RO6806051 (compound 12) is a potent dual inhibitor of fatty acid binding proteins 4 and 5 (FABP4 and FABP5), exhibiting excellent selectivity and absorption, distribution, metabolism, and excretion (eADME) properties.