Chemical Structure : PIPE-307
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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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.
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外观性状 | Solid | |
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Solubility |
10 mM in DMSO |
1. Poon MM, et al. Proc Natl Acad Sci U S A. 2024 Aug 6;121(32):e2407974121.
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