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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-GABA Receptor-MIDD0301
MIDD0301

Chemical Structure : MIDD0301

CAS No.: 2187489-08-1

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MIDD0301 (MIDD 0301, MIDD-0301, GL-II-93)

货号: PC-63310Not For Human Use, Lab Use Only.

MIDD0301 is a potent, positive allosteric, α5β3γ2 selective, GABAA receptor (GABAAR) ligand with EC50 of 17 nM, shows no significant binding at the peripheral GABAAR at 10 uM.

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

生物&药学活性

MIDD0301 (GL-II-93) is a potent, positive allosteric, α5β3γ2 selective, GABAA receptor (GABAAR) ligand with EC50 of 17 nM, shows no significant binding at the peripheral GABAAR at 10 uM.
MIDD0301 causes amplification of GABA induced current mediated by α1-3,5β3γ2 GABAARs in the presence of MIDD0301 in automated patch clamp test.
MIDD0301 relaxes airway smooth muscle at single micromolar concentrations as demonstrated with ex vivo guinea pig tracheal rings, also attenuates airway hyperresponsiveness (AHR) in an ovalbumin murine model of asthma by oral administration, with low brain distribution.
MIDD0301 reduces lung cytokine expression of IL-17A, IL-4, and TNF-α, as wells as the number of CD4+ T cells.

物理化学性质&存储条件

分子量 414.234
分子式 C19H13BrFN3O2
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

(R)-8-bromo-6-(2-fluorophenyl)-4-methyl-4H-benzo[f]imidazo[1,5-a][1,4]diazepine-3-carboxylic acid

参考文献

1. Forkuo GS, et al. Mol Pharm. 2018 Apr 2. doi: 10.1021/acs.molpharmaceut.7b01013.

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