Chemical Structure : PIPE-359
货号: PC-20509Not For Human Use, Lab Use Only.
PIPE-359 (PIPE359) is a potent, selective and brain-penetrant antagonist of muscarinic acetylcholine receptor subtype 1 (M1 mAChR) with IC50 of 1.8 nM and Ki of 0.14 nM (hM1R).
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PIPE-359 (PIPE359) is a potent, selective and brain-penetrant antagonist of muscarinic acetylcholine receptor subtype 1 (M1 mAChR) with IC50 of 1.8 nM and Ki of 0.14 nM (hM1R).
PIPE-359 exhibited good-to-excellent selectivities versus the hM2R, hM3R, and hM4R in both functional and binding settings.
PIPE-359 (30 mg/kg po qd) exhibited robust efficacy in mouse myelin oligodendrocyte glycoprotein (MOG)-induced experimental autoimmune encephalitis (EAE), a preclinical model for multiple sclerosis.
分子量 | 467.56 | |
分子式 | C22H21N5O3S2 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Thomas O Schrader, et al. ACS Med Chem Lett. 2020 Dec 24;12(1):155-161.
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