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PSN375963

Cayman Chemical Item Number 10008593

(CAS 388575-52-8)

PSN375963 (CAS 388575-52-8)

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Description

GPR119 (previously designated SNORF25) is an orphan G protein-coupled receptor expressed predominantly in the pancreas and gastrointestinal tract in humans and in the brain, pancreas, and gastrointestinal tract in rodents. It mediates a reduction in food intake and body weight gain in rats upon treatment with oleoyl ethanolamide (OEA), an endogenous, potent agonist for PPARα.1,2 PSN375963 is a potent and selective agonist of GPR119 that shows similar potency to OEA at both recombinant mouse and human GPR119 receptors, exhibiting EC50 values of 8.4 and 7.9 µM, respectively (EC50 values for OEA are 3.2 and 2.9 µM, respectively).2 These data suggest that PSN375963 may be useful as a therapeutic agent for the treatment of obesity.

1 Fu, J., Gaetani, S., Oveisi, F., et al. Oleylethanolamide regulates feeding and body weight through activation of the nuclear receptor PPAR-α. Nature 425 90-93 (2003).

2 Overton, H.A., Babbs, A.J., Doel, S.M., et al. Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents. Cell Metab 3 167-175 (2006).

Formal Name 4-​[5-​(4-​butylcyclohexyl)-​1,​2,​4-​oxadiazol-​3-​yl]-​pyridine
CAS Number 388575-52-8
Molecular Formula C17H23N3O
Formula Weight 285.4
Formulation A crystalline solid
Purity ≥98%
λmax 224, 273 nm
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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CCCCC1CCC(CC1)​c1onc(n1)​c1ccncc1

Background Reading

Overton, H.A., Babbs, A.J., Doel, S.M., et al. Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents. Cell Metab 3 167-175 (2006).

Fu, J., Gaetani, S., Oveisi, F., et al. Oleylethanolamide regulates feeding and body weight through activation of the nuclear receptor PPAR-α. Nature 425 90-93 (2003).

PSN375963 is available in the following screening library:

Size Price Quantity Subtotal
1 mg $13.00 $0.00
5 mg $59.00 $0.00
10 mg $104.00 $0.00
25 mg $228.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

Please contact our Sales Department for a quote or to purchase.

Pricing updated 2012-05-25. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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