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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-nAChR-DM506
DM506

Chemical Structure : DM506

CAS No.: 7546-66-9

DM506 (DM 506)

货号: PC-21718Not For Human Use, Lab Use Only.

DM506 is a novel ibogamine derivative and inhibitor of α7 and α9α10 nicotinic acetylcholine receptors (nAChRs) with IC50 of 5.1 uM, 5.6 uM and 6.4 uM for α9α10, α7β2 and α7nAChR, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

DM506 is a novel ibogamine derivative and inhibitor of α7 and α9α10 nicotinic acetylcholine receptors (nAChRs) with IC50 of 5.1 uM, 5.6 uM and 6.4 uM for α9α10, α7β2 and α7nAChR, respectively.
DM506 shows no significance differences between rat and human α7 and α9α10 nAChRs.
DM506 shows weak activity against α4β2, α6/α3β2β3 and α3β4 (IC50=25-70 uM).
DM506 inhibits the α7 and α9α10 nAChRs in a voltage-dependent and voltage-independent manner, respectively.
DM506 inhibits both α9α10 and α7 nAChR subtypes by novel allosteric mechanisms likely involving modulation of the extracellular-transmembrane domain junction and cytoplasmic domain.
DM506 induces sedative- and anxiolytic-like activity in mice by a mechanism involving 5-HT2A receptor activation.

物理化学性质&存储条件

分子量 200.29
分子式 C13H16N2
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

3-methyl-1,2,3,4,5,6-hexahydroazepino[4,5-b]indole

参考文献

1. Tae HS, et al. ACS Chem Neurosci. 2023 Jul 19;14(14):2537-2547.

2. Arias HR, et al. Eur J Pharmacol. 2024 Jan 20;966:176329.

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