A cell-permeable, potent, and selective inhibitor of FABP4
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BMS309403

Item No. 10010206

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[2'-(5-ethyl-3,4-diphenyl-1H-pyrazol-1-yl)[1,1'-biphenyl]-3-yl]oxy]-acetic acid
CAS Number
300657-03-8
Synonyms
  • Adipocyte FABP Inhibitor
  • A-FABP Inhibitor
  • ALBP Inhibitor
  • aP2 Inhibitor
  • FABP4 Inhibitor
  • Fatty Acid Binding Protein 4 Inhibitor
Molecular Formula
C31H26N2O3
Formula Weight
474.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 25 mg/mlEthanol: 30 mg/mlEthanol: PBS (pH 7.2) (1:2): 0.3 mg/ml
SMILES
CCC1=C(C2=CC=CC=C2)C(C3=CC=CC=C3)=NN1C4=CC=CC=C4C5=CC=CC(OCC(O)=O)=C5
InChi Code
InChI=1S/C31H26N2O3/c1-2-27-30(22-12-5-3-6-13-22)31(23-14-7-4-8-15-23)32-33(27)28-19-10-9-18-26(28)24-16-11-17-25(20-24)36-21-29(34)35/h3-20H,2,21H2,1H3,(H,34,35)
InChi Key
SJRVJRYZAQYCEE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    25 mg

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    BMS309403 is a cell-permeable, potent inhibitor of FABP4 that targets the fatty acid-binding pocket (Ki < 2 nM).1 It is less effective against FABP3 and FABP5 (Kis = 250 and 350 nM, respectively).1 BMS309403 is orally active, reducing atherosclerosis in mice lacking apoplipoprotein E.2,3 It also protects against the development of insulin resistance associated with genetic or diet-induced obesity in mice.2,4 FABP4 dose-dependently suppresses the release of MCP-1 from macrophages.5,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sulsky, R., Magnin, D.R., Huang, Y., et al. Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP). Bioorg. Med. Chem. Lett. 17(12), 3511-3515 (2007).

    2. Furuhashi, M., Tuncman, G., Görgün, C.Z., et al. Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2. Nature 447, 959-965 (2007).

    3. Lee, M.Y., Li, H., Xiao, Y., et al. Chronic administration of BMS309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells. Br. J. Pharmacol. 162(7), 1564-1576 (2011).

    4. Suhre, K., Römisch-Margl, W., de Angelis, M.H., et al. Identification of a potential biomarker for FABP4 inhibition: The power of lipidomics in preclinical drug testing. J. Biomol. Screen. 16(5), 467-475 (2011).

    5. Lan, H., Cheng, C.C., Kowalski, T.J., et al. Small-molecule inhibitors of FABP4/5 ameliorate dyslipidemia but not insulin resistance in mice with diet-induced obesity. J. Lipid Res. 52(4), 646-656 (2011).