VU6019650

VU6019650 is a potent and selective orthosteric antagonist of M5 mAChR (IC50=36 nM), can be used for opioid use disorder (OUD) relief. VU6019650 can cross blood brain barrier, potentially modulates the mesolimbic dopaminergic reward circuitry. VU6019650 blocks Oxotremorine M iodide (HY-101372A) induced increases of neuronal firing rates of midbrain dopamine neurons in the ventral tegmental area (VTA) [1][2].

Product Specifications

CAS Number

[2926782-31-0]

UNSPSC

12352005

Target

MAChR

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/vu6019650.html

Purity

98.01

Solubility

DMSO : 8.33 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=S(C1=CC2=C(OCC2)C=C1)(N(CC[C@@H]3CSC4=NC=CN4C)C[C@@H]3F)=O

Molecular Formula

C18H22FN3O3S2

Molecular Weight

411.51

References & Citations

[1]Garrison AT, et al. Development of VU6019650: A Potent, Highly Selective, and Systemically Active Orthosteric Antagonist of the M5 Muscarinic Acetylcholine Receptor for the Treatment of Opioid Use Disorder. J Med Chem. 2022 Apr 28;65 (8) :6273-6286.|[2]Capstick RA, et al. Discovery of a potent M5 antagonist with improved clearance profile. Part 1: Piperidine amide-based antagonists. Bioorg Med Chem Lett. 2022 Nov 15;76:128988.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

MAChR5

Available Sizes

Curated Selection

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