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BMS-309403

Catalog No. T4534   CAS 300657-03-8

BMS-309403 is an effective, selective and cell-permeable inhibitor of fatty acid binding protein 4 (FABP4) with a Ki of less than 2 nM.

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BMS-309403 Chemical Structure
BMS-309403, CAS 300657-03-8
Pack Size Availability Price/USD Quantity
2 mg In stock $ 30.00
5 mg In stock $ 48.00
10 mg In stock $ 85.00
25 mg In stock $ 166.00
50 mg In stock $ 216.00
100 mg In stock $ 280.00
1 mL * 10 mM (in DMSO) In stock $ 53.00
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Purity: 99.54%
Purity: 99.52%
Purity: 99.36%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description BMS-309403 is an effective, selective and cell-permeable inhibitor of fatty acid binding protein 4 (FABP4) with a Ki of less than 2 nM.
Targets&IC50 FABP3: 250 nM , FABP4:< 2 nM, FABP5: 350 nM
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[1]. 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[2]. 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[3].
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[4]. 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[2].
Molecular Weight 474.55
Formula C31H26N2O3
CAS No. 300657-03-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 20 mM, Heating is recommended.

DMSO: 50 mg/mL (105.36 mM)

TargetMolReferences and Literature

1. Sulsky R, et al. Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP). Bioorg Med Chem Lett. 2007 Jun 15;17(12):3511-5. 2. Furuhashi M, et al. Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2. Nature. 2007 Jun 21;447(7147):959-65. 3. Lin W, et al. BMS309403 stimulates glucose uptake in myotubes through activation of AMP-activated protein kinase. PLoS One. 2012;7(8):e44570.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Highly Selective Inhibitor Library Bioactive Compounds Library Max Anti-Metabolism Disease Compound Library NO PAINS Compound Library Lipid Metabolism Compound Library Metabolism Compound Library Bioactive Compound Library

Related Products

Related compounds with same targets
FABP4-IN-2

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Keywords

BMS-309403 300657-03-8 Metabolism FABP Inhibitor selective oral Fatty acid-binding protein inhibit BMS 309403 endothelial uptake glucose BMS309403 function inhibitor

 

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