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首页-小分子抑制剂&激动剂-GPCR-mAChR-VU6025733
VU6025733

Chemical Structure : VU6025733

CAS No.:

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VU6025733 (AG06827)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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).

物理化学性质&存储条件

分子量 386.47
分子式 C20H18D5N5O3
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

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

参考文献

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

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