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 |
|---|
| 7-Deoxyloganin
7-Deoxyloganin is a biosynthetic precursor of Loganin. 7-Deoxyloganin undergoes hydroxylation catalyzed by 7-deoxyloganin 7-hydroxylase, a cytochrome P450-dependent monooxygenase, to produce Loganin. |
| Mannose-BSA
Mannose-BSA is an important organic intermediate that combines the properties of mannose and bovine serum albumin, which is of unique value in the field of scientific research, and can be used as a key substance in a variety of organic synthesis reactions. Mannose is an important monosaccharide that binds specifically to mannose receptors (e.g., CD206 receptors on dendritic cells and macrophages), and therefore has a wide range of applications in immunomodulation and targeted drug delivery. BSA is a protein carrier that is commonly used for biocoupling, and its abundant surface amino groups can covalently bind to mannose to form a mannose-BSA complex. |
| Sulfo-NHS-Biotin
Sulfo-NHS-Biotin stongly label single SDS-2ME soluble cuticular protein. |
| GAPDH-IN-1
GAPDH-IN-1 (GAPDH Inhibitor Compound F8) is a covalent inhibitor of GAPDH (IC50 = 39.31 µM). It viability of, and glucose metabolism in, HEK293 cells in a concentration-dependent manner. |
| O-acetylcamptothecin
O-acetylcamptothecin is a derivative of camptothecin, a naturally occurring alkaloid extracted from the bark of the Chinese tree Camptotheca acuminata. Camptothecin and its derivatives are primarily known for their potent anticancer properties, particularly through their action as inhibitors of topoisomerase I, an enzyme critical for DNA replication and transcription. |
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 2010-2024 AbMole BioScience. All Rights Reserved.
