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APD668 (CAS 832714-46-2) LS-H143

GPR119 agonist
LS-H143-1 / 1 mg / $185
LS-H143-5 / 5 mg / $275
LS-H143-10 / 10 mg / $355
USA Shipment Only
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Description: GPR119, a glucose-dependent insulinotropic receptor, is a G protein-coupled receptor that is expressed in pancreatic beta -cells and intestinal L-cells. Activation of GPR119 by the endogenous ligands lyso-phosphatidylcholine (Item No. 10172) and oleoyl ethanolamide increases intracellular cAMP levels and promotes glucose-stimulated insulin secretion. APD668 is a potent agonist of GPR119 (EC50s = 2.7 and 33 nM for human and rat forms, respectively). Chronic dosing with APD668 in Zucker diabetic fatty rats over several weeks significantly reduces blood glucose and glycated hemoglobin levels. H143_ChemicalStructureImage.png
4-[[1-[2-fluoro-4-(methylsulfonyl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-4-yl]oxy]-1-piperidinecarboxylic acid, 1-methylethyl ester
JNJ-28630368
biochemical, chemical, agonist
LS-H143
832714-46-2
C21H24FN5O5S
≥98%
A crystalline solid
 
CC(C)OC(N1CCC(OC2=NC=NC3=C2C=NN3C4=CC=C(S(C)(=O)=O)C=C4F)CC1)=O
InChI=1S/C21H24FN5O5S/c1-13(2)31-21(28)26-8-6-14(7-9-26)32-20-16-11-25-27(19(16)23-12-24-20)18-5-4-15(10-17(18)22)33(3,29)30/h4-5,10-14H,6-9H2,1-3H3
XTRUQJBVQBUKSQ-UHFFFAOYSA-N
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: OSBPL5 related products

Usage Information

APD668 is supplied as a crystalline solid. A stock solution may be made by dissolving the APD668 in the solvent of choice. APD668 is soluble in organic solvents such as DMSO and dimethyl formamide (DMF), which should be purged with an inert gas. The solubility of APD668 in these solvents is approximately 20 and 25 mg/ml, respectively. APD668 is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, APD668 should first be dissolved in DMF and then diluted with the aqueous buffer of choice. APD668 has a solubility of approximately 0.1 mg/ml in a 1:8 solution of DMF:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

References:
  1. 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).
  2. Soga, T., Ohishi, T., Matsui, T., et al. Lysophosphatidylcholine enhances glucose-dependent insulin secretion via an orphan G-protein-coupled receptor. Biochem. Biophys. Res. Commun. 326, 744-751 (2005).
  3. Semple, G., Ren, A., Fioravanti, B., et al. Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control. Bioorg. Med. Chem. Lett. 21(10), 3134-3141 (2011).

 


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