1208222-39-2
Chemical Structure
VU 0365114
- CAS No.: 1208222-39-2
- Formula:C22H14F3NO3
- Molecular Weight:397.35
IUPAC Name: 1-([1,1'-biphenyl]-4-ylmethyl)-5-(trifluoromethoxy)indoline-2,3-dione
InChIKey: SPBGRXOPAXZSER-UHFFFAOYSA-N
SMILES: O=C1N(C2=CC=C(OC(F)(F)F)C=C2C1=O)CC3=CC=C(C4=CC=CC=C4)C=C3
Biological Activity: 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].
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VU 0365114 | 99.33% | 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. | ||||||||||||||||||||
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VU 0365114 (Standard) | VU 0365114 (Standard) is the analytical standard of VU 0365114 (HY-107651). This product is intended for research and analytical applications. 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. | |||||||||||||||||||||
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References
- [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. [Content Brief]
- [2]. Molina J, et al. Control of insulin secretion by cholinergic signaling in the human pancreatic islet. Diabetes. 2014 Aug;63(8):2714-26. [Content Brief]
- [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. [Content Brief]