Product Description: 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].
Formula: C22H14F3NO3
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./[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.
CAS Number: 1208222-39-2
Molecular Weight: 397.35
Compound Purity: 99.41
Research Area: Metabolic Disease
Solubility: DMSO : ≥ 77.5 mg/mL
Target: mAChR
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