VU0119498

VU0119498 is a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM), with EC50s of 6.04, 6.38, and 4.08 µM, respectively. VU0119498 has antidiabetic activity[1][2][3].

Product Specifications

CAS Number

[79183-37-2]

Product Name Alternative

DA-3003-1

UNSPSC

12352005

Hazard Statement

H315, H319, H330

Target

MAChR

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/vu0119498.html

Purity

99.52

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C1N(C2=C(C1=O)C=CC=C2)CC3=CC=C(C=C3)Br

Molecular Formula

C15H10BrNO2

Molecular Weight

316.15

Precautions

H315, H319, H330

References & Citations

[1]Bridges TM, et, al. Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. J Med Chem. 2009 Jun 11;52 (11) :3445-8.|[2]Bridges TM, et, al. Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM. Bioorg Med Chem Lett. 2010 Mar 15;20 (6) :1972-5.|[3]Zhu L, et, al. Allosteric modulation of β-cell M 3 muscarinic acetylcholine receptors greatly improves glucose homeostasis in lean and obese mice. Proc Natl Acad Sci U S A. 2019 Sep 10;116 (37) :18684-18690.