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首页-小分子抑制剂&激动剂-GPCR-mAChR-HTL9936
HTL9936

Chemical Structure : HTL9936

CAS No.: 1438242-59-1

HTL9936 (HTL-9936)

货号: PC-72655Not For Human Use, Lab Use Only.

HTL9936 (HTL-9936) is a potent, selective M1-muscarinic acetylcholine (M1) receptor partial agonist with EC50 of 32 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

HTL9936 (HTL-9936) is a potent, selective M1-muscarinic acetylcholine (M1) receptor partial agonist with EC50 of 32 nM.
HTL9936 dispalys little to no activity against M2 (EC50>20 uM), M3 (EC50>20 uM), M4 (EC50=398 nM).
HTL9936 demonstrated agonist activity in pERK1/2 (EC50=32 nM), label-free dynamic mass redistribution (EC50=79 nM) and inositol phosphate (IP1) assay formats (EC5=631 nM) in CHO cells overexpressing human M1-receptor.
HTL9936 demonstrated no detectable agonism at human M2-, M3-, or M5-receptors, although partial agonist activity was observed at the human M4-receptor.
Co-administration of HTL9936 with scopolamine resulted in a dose-dependent restoration of learning and memory responses, reverses cognitive deficits in a mouse model of neurodegeneration.

物理化学性质&存储条件

分子量 365.518
分子式 C20H35N3O3
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

ethyl (S)-4-(4-((1-methylcyclobutyl)carbamoyl)piperidin-1-yl)azepane-1-carboxylate

参考文献

1. Alastair J H Brown, et al. Cell. 2021 Nov 24;184(24):5886-5901.e22.

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