Synthetic agonist of the orphan GPR119. Although endogenous lipid amides such as oleoyl ethanolamide have been reported to be agonists at GPR119, AR231453 is the first reported high potency agonist (EC50=0.68nM). The compound displayed in vivo activity in rodents and was active in an oral glucose tolerance test in mice following oral administration. AR231453 stimulated the release of GLP-1 via GPR119 receptors in mouse models. It was shown to be a highly selective ligand with no off-target activity across a 76 receptor and enzyme profiling panel (CEREP) and no activity against 140 known and orphan GPCRs in melanophore dispersion assays.
Product Details
| Alternative Name: | 2-Fluoro-4-methanesulfonyl-phenyl)-{6-[4-(3-isopropyl-[1,2,4]oxadiazol-5-yl)-piperidin-1-yl]-5-nitro-pyrimidin-4-yl}-amine |
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| Formula: | C21H24FN7O5S |
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| MW: | 505.5 |
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| CAS: | 733750-99-7 |
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| Purity: | ≥98% (HPLC) |
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| Identity: | Determined by NMR. |
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| Appearance: | Yellow solid. |
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| Solubility: | Soluble in DMSO (>25mg/ml). |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -20°C |
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| Use/Stability: | Store solutions at -20°C for up to 3 months. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Parameterization of the GPR119 receptor agonist AR231453: J. Hamilton, et al.; J. Comput. Chem.
39, 35 (2018),
Abstract;
N-oleoyldopamine enhances glucose homeostasis through the activation of GPR119: Z.L. Chu, et al.; Mol. Endocrinol.
24, 161 (2010),
Abstract;
A role for intestinal endocrine cell-expressed g protein-coupled receptor 119 in glycemic control by enhancing glucagon-like Peptide-1 and glucose-dependent insulinotropic Peptide release: Z.L. Chu, et al.; Endocrinology
149, 2038 (2008),
Abstract;
Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119: G. Semple, et al.; J. Med. Chem.
51, 5172 (2008),
Abstract;
Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents: H.A. Overton, et al.; Cell Metab.
3, 167 (2006),
Abstract;
