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CAY10587 Exclusive

Cayman Chemical Item Number 13143

(CAS 1082058-99-8)

CAY10587 (CAS 1082058-99-8)

See more	Receptor Agonist (48) Diabetes (134) Metabolism (139) Obesity (162)

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	Copy SMILES to clipboard 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:

Bio-active Lipid I Screening Library (96-Well)

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

Pricing updated 2012-02-12. 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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