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Submit ReviewVU 6028418 hydrochloride
Description: Potent and selective M4 mAChR antagonist
Chemical Name: (3aR,5s,6aS)-2-((Tetrahydro-2H-pyran-4-yl)methyl)-N-(6-(2,3,5-trifluorophenyl)pyridazin-3-yl)octahydrocyclopenta[c]pyrrol-5-amine hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for VU 6028418 hydrochloride
VU 6028418 hydrochloride is a potent and selective M4 mAChR antagonist (IC50 = 4.1 nM and 57 nM for human and rat M4 respectively). VU 6028418 hydrochloride dose-dependently reduces the latency to withdraw and reverses cataleptic behavior in haloperidol-treated animals. Orally bioavailable.
Licensing Information
Sold under license from Vanderbilt University
Technical Data for VU 6028418 hydrochloride
| M. Wt | 468.95 |
| Formula | C23H27F3N4O.HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| InChI Key | IQDWZBQDZTVTLN-NESBVOEXSA-N |
| Smiles | [H][C@]12C[C@H](NC3=CC=C(C4=C(C(F)=CC(F)=C4)F)N=N3)C[C@]1(CN(C2)CC5CCOCC5)[H].Cl |
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 6028418 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 46.9 | 100 | |
| ethanol | 23.45 | 50 |
Preparing Stock Solutions for VU 6028418 hydrochloride
The following data is based on the product molecular weight 468.95. 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 |
|---|---|---|---|
| 1 mM | 2.13 mL | 10.66 mL | 21.32 mL |
| 5 mM | 0.43 mL | 2.13 mL | 4.26 mL |
| 10 mM | 0.21 mL | 1.07 mL | 2.13 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.43 mL |
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Product Datasheets for VU 6028418 hydrochloride
References for VU 6028418 hydrochloride
References are publications that support the biological activity of the product.
Spock et al (2021) Discovery of VU6028418: a highly selective and orally bioavailable M4 muscarinic acetylcholine receptor antagonist. ACS Med.Chem.Lett. 12 1342 PMID: 34413964
If you know of a relevant reference for VU 6028418 hydrochloride, please let us know.
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Citations for VU 6028418 hydrochloride
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