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首页-小分子抑制剂&激动剂-GPCR-mAChR-BAY 2413555
BAY 2413555

Chemical Structure : BAY 2413555

CAS No.: 2206665-50-9

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BAY 2413555 (BAY2413555, BAY-2413555)

货号: PC-23358Not For Human Use, Lab Use Only.

BAY 2413555 is a potent, selective positive allosteric modulator of M2 muscarinic acetylcholine receptor (M2 mAChR, M2R) with EC50 of 2.0 nM in functional M2-GIRK assays.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

BAY 2413555 is a potent, selective positive allosteric modulator of M2 muscarinic acetylcholine receptor (M2 mAChR, M2R) with EC50 of 2.0 nM in functional M2-GIRK assays.
BAY 2413555 is a potent positive allosteric modulator with high cooperativity with the endogenous agonist acetylcholine and negligible agonistic activity.
BAY 2413555 shows no significant allosteric effects on other human muscarinic acetylcholine receptors, and has no any agonistic activity on any of the M1-M5 receptors.
BAY 2413555 shows binding Kd of 17 nM for the human M2R in radioligand binding assay.
BAY 2413555 reduced the heart rate in a dose-dependent manner on the heart rate of isolated rat hearts, in the presence of the M2 agonist carbachol.

物理化学性质&存储条件

分子量 584.40
分子式 C23H17F9N4O4
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

7-((3R,4R)-3,4-dihydroxypyrrolidin-1-yl)-6-fluoro-4-oxo-N-((S)-3,3,4,4,4-pentafluorobutan-2-yl)-1-(2,4,6-trifluorophenyl)-1,4-dihydro-1,8-naphthyridine-3-carboxamide

参考文献

1. Vakalopoulos A, et al. J Med Chem. 2024 Oct 28. doi: 10.1021/acs.jmedchem.4c01590.

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