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首页-小分子抑制剂&激动剂-GPCR-mAChR-77-LH-28-1
77-LH-28-1

Chemical Structure : 77-LH-28-1

CAS No.: 560085-11-2

77-LH-28-1

货号: PC-24782Not For Human Use, Lab Use Only.

77-LH-28-1 is a potent, selective, CNS penetrant, and M1 muscarinic receptor agonist, potently stimulates intracellular calcium mobilization in CHO-hM1 cells with pEC50 value of 8.1.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

77-LH-28-1 is a potent, selective, CNS penetrant M1 muscarinic receptor agonist, potently stimulates intracellular calcium mobilization in CHO-hM1 cells with pEC50 value of 8.1.
77-LH-28-1 also is a potent and subtype-selective D4R ligand with pKi of 9.01, >500-fold selective over D2R and D3R.
77-LH-28-1 display high selectivity to activate the M1 mAChR over other mAChR subtypes.
77-LH-28-1 stimulated IP accumulation in CHO-hM1 cell with pEC50 of 7.37.
77-LH-28-1 stimulated cell firing in the CA1 region of the rat hippocampus with pEC50 of 6.3.

物理化学性质&存储条件

分子量 328.50
分子式 C21H32N2O
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

1-[3-(4-butyl-1-piperidinyl)propyl]-3,4-dihydro-2(1H)-quinolinone

参考文献

1. Bonifazi A, et al. J Med Chem. 2014 Nov 13;57(21):9065-77.

2. Langmead CJ, et al. Br J Pharmacol. 2008 Jul;154(5):1104-15.

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