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首页-小分子抑制剂&激动剂-GPCR-mAChR-PIPE-307
PIPE-307

Chemical Structure : PIPE-307

CAS No.:

PIPE-307 (PIPE307)

货号: PC-22795Not For Human Use, Lab Use Only.

PIPE-307 is a potent, selective, orally bioavailable, brain-penetrant antagonist of M1 muscarinic acetylcholine receptor (M1R, M1 mAChR) with Ki of 4.6 nM in membranes overexpressing human M1R.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

PIPE-307 is a potent, selective, orally bioavailable, brain-penetrant antagonist of M1 muscarinic acetylcholine receptor (M1R, M1 mAChR) with Ki of 4.6 nM in membranes overexpressing human M1R.
PIPE-307 displays >10-fold selectivity against membranes overexpressing human M2, M3, M4, or M5 receptors.
PIPE-307 potently inhibits acetylcholine (ACh) induced calcium mobilization using calcium mobilization in M1R overexpressing CHO-K1 cells, >25-fold functional selectivity against other muscarinic isoforms.
PIPE-307 is efficacious in the MOG-EAE mouse model of demyelination/remyelination.

物理化学性质&存储条件

分子量
分子式
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

参考文献

1. Poon MM, et al. Proc Natl Acad Sci U S A. 2024 Aug 6;121(32):e2407974121.

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