VU 6028418 hydrochloride

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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)
Datasheet
Citations
Reviews
Literature (5)

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.

Select a batch to recalculate based on the batch molecular weight:
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

Citations are publications that use Tocris products.

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Literature in this Area

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