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AS-1269574 (CAS 330981-72-1) LS-H71

GPR119 agonist
LS-H71-1 / 1 mg / $175
LS-H71-5 / 5 mg / $215
LS-H71-10 / 10 mg / $225
LS-H71-25 / 25 mg / $305
USA Shipment Only
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Description: GPR119, a glucose-dependent insulinotropic receptor, is a Gs protein-coupled receptor that is expressed in pancreas beta -cells and intestinal L-cells. Activation of GPR119 by the endogenous ligands lyso-phosphatidylcholine and oleoyl ethanolamide increases intracellular cAMP levels and promotes glucose-stimulated insulin secretion. AS-1269574 is an agonist of GPR119 that is effective both in isolated cells and in vivo. It increases cAMP levels in HEK293 cells transfected with human GPR119 (EC50 = 2.5 µM) and glucose-stimulated insulin secretion in mice (100 mg/kg). H71_ChemicalStructureImage.png
2-[[2-(4-bromophenyl)-6-methyl-4-pyrimidinyl]amino]-ethanol
 
biochemical, chemical, agonist
LS-H71
330981-72-1
C13H14BrN3O
≥98%
A solution in ethanol
 
BrC(C=C1)=CC=C1C2=NC(NCCO)=CC(C)=N2
InChI=1S/C13H14BrN3O/c1-9-8-12(15-6-7-18)17-13(16-9)10-2-4-11(14)5-3-10/h2-5,8,18H,6-7H2,1H3,(H,15,16,17)
DUKPGOOUJNUIOI-UHFFFAOYSA-N
Shipped Ambient, store at -20°C, ≥ 1 year 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

AS-1269574 is supplied as a solution in ethanol. To change the solvent, simply evaporate the ethanol under a gentle stream of nitrogen and immediately add the solvent of choice. Solvents such as DMSO and dimethyl formamide purged with an inert gas can be used. The solubility of AS-1269574 in these solvents is approximately 20 mg/ml. AS-1269574 is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, the ethanolic solution of AS-1269574 should be diluted with the aqueous buffer of choice. AS-1269574 has a solubility of approximately 0.1 mg/ml in a 1:10 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. Yoshida, S., Ohishi, T., Matsui, T., et al. Identification of a novel GPR119 agonist, AS1269574, with in vitro and in vivo glucose-stimulated insulin secretion. Biochem. Biophys. Res. Commun. 400, 437-441 (2010).

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