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2187489-08-1

2187489-08-1 structure
2187489-08-1 structure
  • Name: MIDD0301
  • Chemical Name: MIDD0301
  • CAS Number: 2187489-08-1
  • Molecular Formula: C19H13BrFN3O2
  • Molecular Weight: 414.234
  • Catalog: Signaling Pathways Membrane Transporter/Ion Channel GABA Receptor
  • Create Date: 2020-01-11 15:59:51
  • Modify Date: 2024-01-12 20:12:07
  • 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; causes amplification of GABA induced current mediated by α1-3,5β3γ2 GABAARs in the presence of MIDD0301 in automated patch clamp test; 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; reduces lung cytokine expression of IL-17A, IL-4, and TNF-α, as wells as the number of CD4+ T cells.

Name MIDD0301
Description 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; causes amplification of GABA induced current mediated by α1-3,5β3γ2 GABAARs in the presence of MIDD0301 in automated patch clamp test; 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; reduces lung cytokine expression of IL-17A, IL-4, and TNF-α, as wells as the number of CD4+ T cells.
References References 1. Forkuo GS, et al. Mol Pharm. 2018 Apr 2. doi: 10.1021/acs.molpharmaceut.7b01013. View Related Products by Target GABA Receptor
Molecular Formula C19H13BrFN3O2
Molecular Weight 414.234