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CAY10587 Exclusive

Cayman Chemical Item Number 13143

(CAS 1082058-99-8)

CAY10587 (CAS 1082058-99-8)

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Description

The free fatty acid receptor 1 (FFA1/GPR40) is highly expressed in pancreatic β-cells and activated by medium and long-chain fatty acids.1 There is evidence of a link between FFA1/GPR40 and the ability of fatty acids to amplify glucose-stimulated insulin secretion, making this signaling pathway a potential target for regulating diabetes, obesity, and other metabolic disorders.2,3 CAY10587 is a selective FFA1/GPR40 agonist (EC50 = 32 nM) that does not exhibit activity on the related FFA receptors FFA2/GPR43 or FFA3/GPR41.4 At 100 nM, CAY10587 increases glucose-stimulated insulin secretion in the rat insulin-secreting cell line INS-1E.4

1 Briscoe, C.P., Tadayyon, M., Andrews, J.L., et al. The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids. J Biol Chem 278(13) 11303-11311 (2003).

2 Itoh, Y., Kawamata, Y., Harada, M., et al. Free fatty acids regulate insulin secretion from pancreatic b cells through GPR40. Nature 422 173-176 (2003).

3 Steneberg, P., Rubins, N., Bartoov-Shifman, R., et al. The FFA receptor GPR40 links hyperinsulinemia, hepatic steatosis, and impaired glucose homeostasis in mouse. Cell Metab 1 245-258 (2005).

4 Christiansen, E., Urban, C., Merten, N., et al. Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA1/GPR40), a potential target for the treatment of type II diabetes. J Med Chem 51 7061-7064 (2008).

Formal Name 4-​[2-​(2-​methylphenyl)ethynyl]-​benzenepropanoic acid
CAS Number 1082058-99-8
Molecular Formula C18H16O2
Formula Weight 264.3
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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CC1=C(C#CC2=CC=C(CCC(O)​=O)​C=C2)​C=CC=C1

Background Reading

Briscoe, C.P., Tadayyon, M., Andrews, J.L., et al. The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids. J Biol Chem 278(13) 11303-11311 (2003).

Itoh, Y., Kawamata, Y., Harada, M., et al. Free fatty acids regulate insulin secretion from pancreatic b cells through GPR40. Nature 422 173-176 (2003).

Steneberg, P., Rubins, N., Bartoov-Shifman, R., et al. The FFA receptor GPR40 links hyperinsulinemia, hepatic steatosis, and impaired glucose homeostasis in mouse. Cell Metab 1 245-258 (2005).

Christiansen, E., Urban, C., Merten, N., et al. Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA1/GPR40), a potential target for the treatment of type II diabetes. J Med Chem 51 7061-7064 (2008).

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CAY10587 is available in the following screening library:

Size Price Quantity Subtotal
1 mg $26.00 $0.00
5 mg $117.00 $0.00
10 mg $208.00 $0.00
25 mg $455.00 $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 2012-05-26. 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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