VU6008055 | M4 mAChR PAM | Probechem Biochemicals

Chemical Structure : VU6008055

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VU6008055 (AF98943)

货号: PC-24879Not For Human Use, Lab Use Only.

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100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	379.48
分子式	C20H21N5OS
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-(4-(((3,4-dimethylpyrimido[4',5':4,5]thieno[2,3-c]pyridazin-8-yl)amino)methyl)phenyl)propan-2-ol

参考文献

1. Engers JL, et al. ACS Chem Neurosci. 2025 Jun 4;16(11):2141-2162.

VU6008055 (AF98943)

生物&药学活性

物理化学性质&存储条件

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VU6008055 (AF98943)

生物&药学活性

物理化学性质&存储条件

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