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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-nAChR-BNC375
BNC375

Chemical Structure : BNC375

CAS No.: 1557240-80-8

BNC375 (BNC-375)

货号: PC-73023Not For Human Use, Lab Use Only.

BNC375 (BNC-375) is a potent, selective, orally available type I α7 nAChR positive allosteric modulator (PAM) with EC50 of 1.3 uM.

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

生物&药学活性

BNC375 (BNC-375) is a potent, selective, orally available type I α7 nAChR positive allosteric modulator (PAM) with EC50 of 1.3 uM.
BNC375 significantly potentiated the acetylcholine signal without changing the rapid receptor desensitization.
BNC375 exhibited the MED of 0.03 mg/kg, and full reversal of the scopolamine-induced impairment was achieved at 1.0 mg/kg in mouse T-maze model.
BNC375 possessed an excellent safety profile: no change in the spatial and temporal response of the receptor to endogenous ligand ACh, no activity on other related channels, and no inhibition of major drug metabolizing enzymes such as CYP3A4, CYP2C9, CYP2D6, CYP1A2, and CYP2C19 (IC50 >10 uM).

物理化学性质&存储条件

分子量 394.914
分子式 C19H23ClN2O3S
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

4-((1R,3R)-3-(((5-chloro-2-methoxyphenyl)amino)methyl)-2,2-dimethylcyclopropyl)benzenesulfonamide

参考文献

1. Harvey AJ, et al. ACS Med Chem Lett. 2019 Mar 25;10(5):754-760.

2. Wang X, et al. J Pharmacol Exp Ther. 2020 May;373(2):311-324.

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