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BMS 309403

Cat. No. M6265

All AbMole products are for research use only, cannot be used for human consumption.

BMS 309403 Structure
Size Price Availability Quantity
5mg USD 60  USD60 In stock
10mg USD 110  USD110 In stock
25mg USD 220  USD220 In stock
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Quality Control & Documentation
Biological Activity

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.

Protocol (for reference only)
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.
Chemical Information
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
References

[1] Boss M, et al. Atherosclerosis. FABP4 inhibition suppresses PPARγ activity and VLDL-induced foam cell formation in IL-4-polarized human macrophages.

[2] Hoo RL, et al. J Hepatol. Pharmacological inhibition of adipocyte fatty acid binding protein alleviates both acute liver injury and non-alcoholic steatohepatitis in mice.

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Keywords: BMS 309403 supplier, inhibitors, activators

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