VU 0365114

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].

Product Specifications

CAS Number

[1208222-39-2]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

MAChR

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/VU_0365114.html

Concentration

10mM

Purity

99.41

Solubility

DMSO : ≥ 77.5 mg/mL

Smiles

O=C1N(C2=CC=C(OC(F)(F)F)C=C2C1=O)CC3=CC=C(C4=CC=CC=C4)C=C3

Molecular Formula

C22H14F3NO3

Molecular Weight

397.35

Precautions

H302, H315, H319, H335

References & Citations

[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.