AR231453 (CAS 733750-99-7)
Alternate Names:
2-Fluoro-4-methanesulfonyl-phenyl)-{6-[4-(3-isopropyl-[1,2,4]oxadiazol-5-yl)-piperidin-1-yl]-5-nitro-pyrimidin-4-yl}-amine
CAS Number:
733750-99-7
Molecular Weight:
505.52
Molecular Formula:
C21H24FN7O5S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
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.
AR231453 (CAS 733750-99-7) References
- Structural basis for constitutive activity and agonist-induced activation of the enteroendocrine fat sensor GPR119. | Engelstoft, MS., et al. 2014. Br J Pharmacol. 171: 5774-89. PMID: 25117266
- Biased signaling of lipids and allosteric actions of synthetic molecules for GPR119. | Hassing, HA., et al. 2016. Biochem Pharmacol. 119: 66-75. PMID: 27569424
- GPR119, a Major Enteroendocrine Sensor of Dietary Triglyceride Metabolites Coacting in Synergy With FFA1 (GPR40). | Ekberg, JH., et al. 2016. Endocrinology. 157: 4561-4569. PMID: 27779915
- β-Cell Inactivation of Gpr119 Unmasks Incretin Dependence of GPR119-Mediated Glucoregulation. | Panaro, BL., et al. 2017. Diabetes. 66: 1626-1635. PMID: 28254842
- Parameterization of the GPR119 Receptor Agonist AR231453. | Hamilton, J. and Kotsikorou, E. 2018. J Comput Chem. 39: 35-41. PMID: 29023843
- Bidirectional GPR119 Agonism Requires Peptide YY and Glucose for Activity in Mouse and Human Colon Mucosa. | Tough, IR., et al. 2018. Endocrinology. 159: 1704-1717. PMID: 29471473
- One-pot synthesis of novel tert-butyl-4-substituted phenyl-1H-1,2,3-triazolo piperazine/piperidine carboxylates, potential GPR119 agonists. | Bashetti, N., et al. 2019. Bioorg Med Chem Lett. 29: 126707. PMID: 31630858
- Intestine-selective reduction of Gcg expression reveals the importance of the distal gut for GLP-1 secretion. | Panaro, BL., et al. 2020. Mol Metab. 37: 100990. PMID: 32278655
- GPCRs get fatty: the role of G protein-coupled receptor signaling in the development and progression of nonalcoholic fatty liver disease. | Kurtz, R., et al. 2021. Am J Physiol Gastrointest Liver Physiol. 320: G304-G318. PMID: 33205999
- Long-Acting Glucagon-Like Peptide-1 Receptor Agonists Suppress Voluntary Alcohol Intake in Male Wistar Rats. | Marty, VN., et al. 2020. Front Neurosci. 14: 599646. PMID: 33424537
- GPR119 and GPR55 as Receptors for Fatty Acid Ethanolamides, Oleoylethanolamide and Palmitoylethanolamide. | Im, DS. 2021. Int J Mol Sci. 22: PMID: 33494185
- Targeting the GPR119/incretin axis: a promising new therapy for metabolic-associated fatty liver disease. | Zhao, J., et al. 2021. Cell Mol Biol Lett. 26: 32. PMID: 34233623
- Activation and signaling mechanism revealed by GPR119-Gs complex structures. | Qian, Y., et al. 2022. Nat Commun. 13: 7033. PMID: 36396650
- Intestinal GPR119 activation by microbiota-derived metabolites impacts feeding behavior and energy metabolism. | Igarashi, M., et al. 2023. Mol Metab. 67: 101649. PMID: 36462626
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
AR231453, 5 mg | sc-471106 | 5 mg | $87.00 |