PSN632408

• CAT Number: I005154
• CAS Number: 857652-30-3
• Molecular Formula: C18H24N4O4
• Molecular Weight: 360.4
• Purity: ≥95%
• Synonyms: 4-[[3-(4-pyridinyl)-1,2,4-oxadiazol-5-yl]methoxy]-1-piperidinecarboxylic acid, 1,1-dimethylethyl ester
• Target: Neuronal Signaling
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 5.6/7.9 uM ( recombinant mouse/ human GPR119) [1]
• InChIKey: LHZWKWCEAXQUMX-UHFFFAOYSA-N
• SMILES: O=C(OC(C)(C)C)N1CCC(OCc2onc(n2)c2ccncc2)CC1

PSN632408 (CAT: I0051543) is an optimized agonist of GPR119 receptors, which are involved in glucose homeostasis and insulin secretion. It has been found to exhibit similar potency to OEA (oleoylethanolamide) at both recombinant mouse and human GPR119 receptors, with EC50 values of 5.6 and 7.9 μM, respectively. As an agonist, PSN632408 activates GPR119 receptors, leading to the release of incretin hormones and enhanced glucose-dependent insulin secretion. This compound holds the potential for the development of therapeutic agents targeting GPR119 receptors to regulate glucose metabolism and potentially treat conditions such as type 2 diabetes mellitus.

Reference

1: Cornall LM, Hryciw DH, Mathai ML, McAinch AJ. Direct activation of the proposed anti-diabetic receptor, GPR119 in cardiomyoblasts decreases markers of muscle metabolic activity. Mol Cell Endocrinol. 2015 Feb 15;402:72-85. doi: 10.1016/j.mce.2015.01.006. Epub 2015 Jan 8. PubMed PMID: 25578601.
2: Panaro BL, Tough IR, Engelstoft MS, Matthews RT, Digby GJ, Møller CL, Svendsen B, Gribble F, Reimann F, Holst JJ, Holst B, Schwartz TW, Cox HM, Cone RD. The melanocortin-4 receptor is expressed in enteroendocrine L cells and regulates the release of peptide YY and glucagon-like peptide 1 in vivo. Cell Metab. 2014 Dec 2;20(6):1018-29. doi: 10.1016/j.cmet.2014.10.004. Epub 2014 Nov 20. PubMed PMID: 25453189; PubMed Central PMCID: PMC4255280.
3: Ansarullah, Lu Y, Holstein M, DeRuyter B, Rabinovitch A, Guo Z. Stimulating β-cell regeneration by combining a GPR119 agonist with a DPP-IV inhibitor. PLoS One. 2013;8(1):e53345. doi: 10.1371/journal.pone.0053345. Epub 2013 Jan 29. PubMed PMID: 23382843; PubMed Central PMCID: PMC3558424.
4: Cornall LM, Mathai ML, Hryciw DH, Simcocks AC, O/’Brien PE, Wentworth JM, McAinch AJ. GPR119 regulates genetic markers of fatty acid oxidation in cultured skeletal muscle myotubes. Mol Cell Endocrinol. 2013 Jan 5;365(1):108-18. doi: 10.1016/j.mce.2012.10.003. Epub 2012 Oct 13. PubMed PMID: 23069642.
5: Gao J, Tian L, Weng G, Bhagroo NV, Sorenson RL, O/’Brien TD, Luo J, Guo Z. Stimulating beta cell replication and improving islet graft function by GPR119 agonists. Transpl Int. 2011 Nov;24(11):1124-34. doi: 10.1111/j.1432-2277.2011.01332.x. Epub 2011 Sep 8. PubMed PMID: 21902730.