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首页-小分子抑制剂&激动剂-GPCR-mAChR-VU0467319
VU0467319

Chemical Structure : VU0467319

CAS No.: 1432438-14-6

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VU0467319 (VU319)

货号: PC-23641Not For Human Use, Lab Use Only.

VU0467319 (VU319) is a potent, selective and CNS penetrant M1 mAChR positive allosteric modulator (PAM) with EC50 of 492 nM, with minimal M1 agonism (EC50 > 30 uM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

VU0467319 (VU319) is a potent, selective and CNS penetrant M1 mAChR positive allosteric modulator (PAM) with EC50 of 492 nM, with minimal M1 agonism (EC50 > 30 uM).
VU0467319 (VU319) potentiates M1 in all three species: rat (M1 EC50 = 398 nM, 81.3 ± 11.3% ACh Max), mouse (M1 EC50 = 728 nM, 55.9 ± 5.6% ACh Max) and cyno (M1 EC50 = 374 nM, 57.8% ACh max).
VU0467319 (VU319) is ineffective in shifting ACh affinity at rat M2, M3, M4 or M5 receptors.
VU0467319 (VU319) potentiates the recruitment of β-arrestin2 to the human M1 receptor in a concentration dependent manner (EC50 = 890 nM, 72% max).
VU0467319 (VU319) also potentiates the response of oxotremorine-M (M1 EC50 = 400 nM, 59% ACh Max, M2–5 EC50 > 30 μM), but was ineffective at potentiating xanomeline, clozapine or N-desmethylclozapine (NDMC).
VU0467319 (VU319) demonstrated the feasibility of achieving selective targeting of central M1 muscarinic receptors without eliciting cholinergic AEs that have plagued other drugs targeting CNS cholinergic neurotransmission.

物理化学性质&存储条件

分子量 390.39
分子式 C22H16F2N4O
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-(2,6-difluoro-4-(2-methyl-2H-indazol-4-yl)benzyl)-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-5-one

参考文献

1. Poslunsey MS, et al. ACS Chem Neurosci. 2024 Dec 11. doi: 10.1021/acschemneuro.4c00769.

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