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VU6025733

Chemical Structure : VU6025733

CAS No.:

VU6025733 (AG06827)

Catalog No.: PC-26253Not For Human Use, Lab Use Only.

VU6025733 (AG06827) is a highly selective, orally bioavailable M4 muscarinic acetylcholine receptor (M4 mAChR) positive allosteric modulator (PAM) with EC50 of 23 nM and 55 nM for hM4 and rM4 respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

VU6025733 (AG06827) is a highly selective, orally bioavailable M4 muscarinic acetylcholine receptor (M4 mAChR) positive allosteric modulator (PAM) with EC50 of 23 nM and 55 nM for hM4 and rM4 respectively.
VU6025733 exhibited no appreciable species differences in M4 activity between human and rat (∼2-fold).
VU6025733 is inactive against other subtypes of muscarinic acetylcholine receptors (M1, M2, M3, and M5).
VU6025733 demonstrated a robust dose-dependent blockade of amphetamine-induced hyperlocomotion (AHL) after oral administration following a 30 min pretreatment interval in rats (MED=10 mg/kg).

Physicochemical Properties

M.Wt 386.47
Formula C20H18D5N5O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-(4-((2,3-Dihydrobenzo­[b]­[1,4]­dioxin-6-yl-2,2,3,3-d4)­oxy)­piperidin-1-yl-4-d)-7,8-dimethyl-[1,2,4]­triazolo­[4,3-b]­pyridazine

References

1. Gregro AR, et al. ACS Chem Neurosci. 2026 Feb 4;17(3):649-665.

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