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VU6019650

CAT: 0804-HY-148502-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-148502-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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 induced increases of neuronal firing rates of midbrain dopamine neurons in the ventral tegmental area (VTA)[2].
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

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CatalogName
BA5496-5VU6019650

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