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BMS-309403

AG-CR1-3640-M001 1 mg INQ
AG-CR1-3640-M005 5 mg INQ
AG-CR1-3640-M025 25 mg INQ
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Additional Information

Product Data
Synonyms BMS309403; BMS 309403; FABP4 Inhibitor; 2-[[2'-(5-Ethyl-3,4-diphenyl-1H-pyrazol-1-yl)[1,1'-biphenyl]-3-yl]oxy]acetic acid
Properties
Formula C31H26N2O3
MW 474.6
CAS 300657-03-8
Purity ≥98% (HPLC)
Appearance White to off-white solid.
Solubility Soluble in DMSO (25mg/ml), ethanol (30mg/ml), dimethylformamide (30mg/ml) or methanol. Almost insoluble in water.
Identity Determined by 1H-NMR.
InChi Key SJRVJRYZAQYCEE-UHFFFAOYSA-N
Product Type Chemical
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Handling Advice Keep cool and dry. Protect from moisture.
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
Documents
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Product Description

  • Cell permeable, potent and selective fatty acid binding protein 4 (FABP4; A-FABP; ALBP; adipocyteP2 protein) inhibitor that competitively targets the fatty acid-binding pocket (Ki= <2nM). Inhibits FABP3 (muscle) and FABP5 (epidermal) with lower affinity (Ki=250nM and 350nM, respectively). FABP4 is an intracellular lipid-binding protein responsible for the transportation of fatty acids. It is expressed primarily in adipose tissue and is associated with inflammation, obesity, diabetes and cardiovascular diseases.
  • Glucose uptake stimulator. Reduces blood glucose levels and increases insulin sensitivity in a mouse model of obesity. Protects against the development of insulin resistance associated with genetic or diet-induced obesity in mice.
  • Anti-atherosclerotic. Decreases fatty acid uptake in adipocytes in vitro and reduces atherosclerotic lesion area in a mouse model of atherosclerosis.

Product References

  1. Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP): R. Sulsky, et al.; Bioorg. Med. Chem. Lett. 17, 3511 (2007)
  2. Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2: M. Furuhashi, et al.; Nature 447, 959 (2007)
  3. BMS309403 stimulates glucose uptake in myotubes through activation of AMP-activated protein kinase: W. Lin, et al.; PLoS One 7, e44570 (2012)
  4. FABP4 attenuates PPARγ and adipogenesis and is inversely correlated with PPARγ in adipose tissues: T. Garin-Shkolnik, et al.; Diabetes 63, 900 (2014)
  5. FABP4 inhibition suppresses PPARγ activity and VLDL-induced foam cell formation in IL-4-polarized human macrophages: M. Boss, et al.; Atherosclerosis 240, 424 (2015)
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