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PSN632408 Exclusive

Cayman Chemical Item Number 10008594

(CAS 857652-30-3)

PSN632408 (CAS 857652-30-3)

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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 PSN632408 is an optimized agonist of GPR119 receptors that shows similar potency to OEA at both recombinant mouse and human GPR119 receptors, exhibiting EC50 values of 5.6 and 7.9 µM, respectively (EC50 values for OEA are 3.2 and 2.9 µM, respectively).2 Systemic administration of PSN632408 (30 mg/kg intraperitoneally) suppresses food intake, reduces weight gain, and white adipose tissue deposition in rats.2 These data suggest that PSN632408 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-​[[3-​(4-​pyridinyl)-​1,​2,​4-​oxadiazol-​5-​yl]methoxy]-​1-​piperidinecarboxylic acid,​ 1,​1-​dimethylethyl ester
CAS Number 857652-30-3
Molecular Formula C18H24N4O4
Formula Weight 360.4
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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O=C(OC(C)​(C)​C)​N1CCC(OCc2onc(n2)​c2ccncc2)​CC1

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).

PSN632408 is available in the following screening library:

Size Price Quantity Subtotal
1 mg $21.00 $0.00
5 mg $95.00 $0.00
10 mg $168.00 $0.00
25 mg $368.00 $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.

To ask for assistance with one of our products please contact a Technical Support Scientist.

Warning This product is not for human or veterinary use.

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