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CPL207280

Chemical Structure : CPL207280

CAS No.: 2361497-72-3

CPL207280 (CPL 207280)

Catalog No.: PC-72119Not For Human Use, Lab Use Only.

CPL207280 (CPL 207280) is a novel potent, selective GPR40/FFA1 agonist with EC50 of 80 nM in a Ca2+ influx assay, shows greater potency than fasiglifam (EC50=270 nM).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

CPL207280 (CPL 207280) is a novel potent, selective GPR40/FFA1 agonist with EC50 of 80 nM in a Ca2+ influx assay, shows greater potency than fasiglifam (EC50=270 nM).
CPL207280 did not demonstrate any activity on the related GPR receptors, i.e., GPR41 (FFA2), GPR43 (FFA3), GPR55, GPR119, GPR120, GPR142, PPARα, or PPARγ at 10 uM.
At 10 uM, CPL207280 showed 3.9 times greater enhancement of glucose-stimulated insulin secretion in mouse MIN6 pancreatic β-cells.
CPL207280 improved glucose tolerance and increased insulin area in diabetic rats. CPL207280 is a potent enhancer of glucose-stimulated insulin secretion in animal disease models with no risk of hypoglycemia at therapeutic doses.

Physicochemical Properties

M.Wt 286.371
Formula C18H22O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-3-(4-((2,3-dimethylbut-2-en-1-yl)oxy)phenyl)hex-4-ynoic acid

References

1. Bazydlo-Guzenda K, et al. Mol Pharmacol. 2021 Oct;100(4):335-347.

2. Smuga D, et al. Eur J Med Chem. 2021 Dec 15;226:113810.

3. Bazydlo-Guzenda K, et al. PLoS One. 2021 Sep 23;16(9):e0257477.

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