For research use only. Not for therapeutic Use.
VU 0365114 is a selective mAChR M5 positive allosteric modulator, with an EC50 of 2.7 μM, and >30 μM for M1, M2, M3 and M4 receptors. VU 0365114 increases insulin secretion stimulated by ACh in human β-cells[1][2][3].
VU 0365114 (10 μM) increases insulin secretion stimulated by ACh in human β-cells[2].
VU 0365114 (10 μM) does not alter somatostatin secretion stimulated by ACh in human β-cells[2].
| Catalog Number | R059567 |
| CAS Number | 1208222-39-2 |
| Synonyms | 1-[(4-phenylphenyl)methyl]-5-(trifluoromethoxy)indole-2,3-dione |
| Molecular Formula | C22H14F3NO3 |
| Purity | ≥95% |
| InChI | InChI=1S/C22H14F3NO3/c23-22(24,25)29-17-10-11-19-18(12-17)20(27)21(28)26(19)13-14-6-8-16(9-7-14)15-4-2-1-3-5-15/h1-12H,13H2 |
| InChIKey | SPBGRXOPAXZSER-UHFFFAOYSA-N |
| SMILES | C1=CC=C(C=C1)C2=CC=C(C=C2)CN3C4=C(C=C(C=C4)OC(F)(F)F)C(=O)C3=O |
| Reference | [1]. Bridges TM, et al. Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5617-22. [2]. Molina J, et al. Control of insulin secretion by cholinergic signaling in the human pancreatic islet. Diabetes. 2014 Aug;63(8):2714-26. [3]. Bridges TM, et al. Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM. Bioorg Med Chem Lett. 2010 Jan 15;20(2):558-62. |
