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首页-小分子抑制剂&激动剂-GPCR-Sigma Receptor-AF710B
AF710B

Chemical Structure : AF710B

CAS No.: 3111245-04-3

AF710B ((S)-AF710)

货号: PC-28113Not For Human Use, Lab Use Only.

AF710B ((S)-AF710) is a highly potent and selective allosteric M1 muscarinic and σ1 receptor (M1 mAChR/σ1R) agonist.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

AF710B ((S)-AF710) is a highly potent and selective allosteric M1 muscarinic and σ1 receptor (M1 mAChR/σ1R) agonist.
AF710B significantly potentiates the binding and efficacy of carbachol on M1 receptors and their downstream effects (p-ERK1/2, p-CREB).
AF710B binds with high affinity to M1 mAChR showing an allosteric agonistic profile.
AF710B binds with high affinity to σ1R and does not bind to σ2R (IC50> 10 μM).
AF710B potentiates the effects induced by carbachol and improves cognition in a passive avoidance test in trihexyphenidyl-treated rats.
AF710B shows exceptional efficacy in restoring cognitive decline associated with AD and with lessening BACE1, GSK3β activity, p25CDK5, neuroinflammation, soluble and insoluble Aβ40, Aβ42, accumulation of amyloid plaques and neurofibrillary tangles.

物理化学性质&存储条件

分子量 357.52
分子式 C20H27N3OS
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

(S)-1-(2,8-dimethyl-1-thia-3,8-diazaspiro[4.5]decan-3-yl)-3-(1H-indol-3-yl)propan-1-one

参考文献

1. Fisher A, et al. Neurodegener Dis. 2016;16(1-2):95-110.

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