VU 0365114_product_DataBase

Bioactivity

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].

Invitro

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].

Name

VU 0365114

CAS

1208222-39-2

Formula

C22H14F3NO3

Molar Mass

397.35

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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.

PeptideDB

VU 0365114

CAS: 1208222-39-2 F: C22H14F3NO3 W: 397.35