Chemical Structure : VU6008055
CAS No.:
2170551-59-2
VU6008055
(AF98943)
Catalog No.: PC-24879Not For Human Use, Lab Use Only.
VU6008055 (AF98943) is a potent, highly selective, orally bioavailable M4 muscarinic acetylcholine receptor positive allosteric modulator with EC50 of 73.4 nM and 19.5 nM for human and rat M4 receptor respectively.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
VU6008055 (AF98943) is a potent, highly selective, orally bioavailable M4 muscarinic acetylcholine receptor positive allosteric modulator with EC50 of 73.4 nM and 19.5 nM for human and rat M4 receptor respectively.
VU6008055 displays high subtype selectivity across the human mAChRs (M1, M3, and M5 = inactive; M2 = 41-fold selectivity) in addition to exhibiting no appreciable species differences in M4 activity.
VU6008055 completely displaced the binding of the M4 subtype-selective radioligand [3H]MK-6884 at both human and rat M4 with Ki of 40 nM and 18 nM respectively.
VU6008055 is highly brain penetrant, has an overall superior pharmacological and DMPK profile to previously reported M4 PAMs, and demonstrates efficacy in preclinical models of antipsychotic-like activity.
Physicochemical Properties
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M.Wt
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379.48
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Formula
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C20H21N5OS
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2-(4-(((3,4-dimethylpyrimido[4',5':4,5]thieno[2,3-c]pyridazin-8-yl)amino)methyl)phenyl)propan-2-ol
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References
1. Engers JL, et al. ACS Chem Neurosci. 2025 Jun 4;16(11):2141-2162.
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