VU 0365114
Product Specifications
UNSPSC 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].
Target Antigen
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
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 Weight
397.35
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-107651/VU-0365114-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-107651/VU-0365114-SDS-MedChemExpress.pdf
Clinical Information
No Development Reported
CAS Number
1208222-39-2
Available Sizes
Curated Selection
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