All AbMole products are for research use only, cannot be used for human consumption.
In vitro: BMS-309403 binds to FABP4 with high affinity and shows over 100-fold selectivity against FABP5 as well as the heart isoform FABP3. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. Treatment with BMS-309403 significantly decreased MCP-1 production from THP-1 macrophages in a dose- and time-dependent manner. BMS-309403 stimulates glucose uptake in C2C12 myotubes in a temporal and dose dependent manner via activation of AMP-activated protein kinase (AMPK) signaling pathway but independent of FABPs.
In vivo: A 6 week treatment with BMS-309403 improves endothelial function, phosphorylated and total eNOS and reduced plasma triglyceride levels but does not affect endothelium-independent relaxations. In cultured human microvascular endothelial cells, lipid-induced A-FABP expression is associated with reduced phosphorylated eNOS and NO production and is reversed by BMS-309403. The extent of atherosclerotic lesion area in the proximal aorta is significantly reduced in the BMS-309403-treated group compared with vehicle-treated controls in both the early and late intervention studies.
| Cell Experiment | |
|---|---|
| Cell lines | IL-4-stimulated cells |
| Preparation method | LPL expression correlated with increased very low density lipoprotein (VLDL)- induced triglyceride accumulation in IL-4-polarized macrophages, which was sensitive to inhibition of lipolysis or PPARg antagonism. Inhibition of FABP4 during differentiation using chemical inhibitors BMS309403 and HTS01037 or FABP4 siRNA decreased the expression of FABP4 and LPL, and reduced lipid accumulation in macrophages treated with VLDL. |
| Concentrations | 50 mM |
| Incubation time | 6 h |
| Animal Experiment | |
|---|---|
| Animal models | C57BL/6J male mice |
| Formulation | PBS |
| Dosages | 15 mg/kg/day |
| Administration | i.v. |
| Molecular Weight | 474.55 |
| Formula | C31H26N2O3 |
| CAS Number | 300657-03-8 |
| Solubility (25°C) | 62.5 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Products |
|---|
| Lactate calcium
Lactate calcium is an excellent calcium fortifier that works better than inorganic calcium. Lactate calcium is used as an antacid. |
| Coniferyl ferulate
Coniferyl ferulate is a potent glutathione S-transferase (GST) inhibitor that reverses multidrug resistance and down-regulates p-glycoprotein. Coniferyl ferulate strongly inhibited human placental glutathione S-transferase with IC50 of 0.3 μM. |
| NXY-059
NXY-059 is a free radical-trapping neuroprotectant that has been reported to reduce infarct size and preserve brain function in experimental models of acute ischemic stroke. |
| Tie2 kinase inhibitor
Tie2 kinase inhibitor is a potent, reversible, and ATP-binding site-targeting Tie2 inhibitor with an IC50 of 250 nM. |
| Calcium levofolinate
Calcium levofolinate is a calcium salt of folinic acid that is an adjuvant used in cancer chemotherapy. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
