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Submit ReviewVU 6019650
Description: M5 receptor antagonist
Chemical Name: (3R,4S)-rel-1-[(2,3-Dihydro-5-benzofuranyl)sulfonyl]-3-fluoro-4-[[(1-methyl-1H-imidazol-2-yl)thio]methyl]piperidine
Purity: ≥98% (HPLC)
Biological Activity for VU 6019650
VU 6019650 is a potent and selective M5 receptor antagonist (hM5 IC50 = 36 nM). Exhibits >100-fold selectivity over human and rat M1-4. In vivo, VU 6019650 inhibits the reward effects of oxycodone and reduces oxycodone self-administration in rats. VU 6019650 is blood brain barrier penetrant.
Licensing Information
Sold under license from Vanderbilt University
Technical Data for VU 6019650
| M. Wt | 411.51 |
| Formula | C18H22FN3O3S2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2926782-31-0 |
| PubChem ID | 164673826 |
| InChI Key | MWXZKSDFCSPEBK-ZBFHGGJFSA-N |
| Smiles | O=S(C1=CC=C(OCC2)C2=C1)(N3C[C@@H]([C@H](CC3)CSC4=NC=CN4C)F)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for VU 6019650
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 20.58 | 50 |
Preparing Stock Solutions for VU 6019650
The following data is based on the product molecular weight 411.51. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 4.86 mL | 24.3 mL | 48.6 mL |
| 2.5 mM | 0.97 mL | 4.86 mL | 9.72 mL |
| 5 mM | 0.49 mL | 2.43 mL | 4.86 mL |
| 25 mM | 0.1 mL | 0.49 mL | 0.97 mL |
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Product Datasheets for VU 6019650
References for VU 6019650
References are publications that support the biological activity of the product.
Garrison et al (2022) 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. 65 6273 PMID: 35417155
Capstick et al (2022) Discovery of a potent M5 antagonist with improved clearance profile. Part 1: Piperidine amide-based antagonists. Bioorg.Med.Chem.Lett. 76 128988 PMID: 36113671
If you know of a relevant reference for VU 6019650, please let us know.
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Keywords: VU 6019650, VU 6019650 supplier, VU6019650, acetylcholine, muscarinic, machrs, receptors, m5, Antagonist, antagonists, potent, selective, bbb, blood, brain, barrier, oxycodone, in, vivo, M5, Receptors, 8055, Tocris Bioscience
Citations for VU 6019650
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