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GAT107

Catalog No. T27404   CAS 1476807-74-5
Synonyms: GAT 107, GAT-107

GAT107 is a novel and potent α7 nicotinic cholinergic receptor modifier agonist and modulator with anti-inflammatory activity that reverses injury perception in a mouse model of neuropathic pain.

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GAT107 Chemical Structure
GAT107, CAS 1476807-74-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 258.00
5 mg In stock $ 642.00
10 mg In stock $ 913.00
25 mg In stock $ 1,370.00
50 mg In stock $ 1,850.00
100 mg In stock $ 2,500.00
500 mg In stock $ 4,900.00
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Purity: 98.76%
ee: 100%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GAT107 is a novel and potent α7 nicotinic cholinergic receptor modifier agonist and modulator with anti-inflammatory activity that reverses injury perception in a mouse model of neuropathic pain.
In vitro The incubation of macrophages with 3.3 μM of GAT107 significantly decreased hyperoxia-induced extracellular HMGB1 accumulation and HMGB1-induced macrophage phagocytic dysfunction. Hyperoxia-compromised macrophage function was correlated with impaired mitochondrial membrane integrity, increased superoxide levels, and decreased manganese superoxide dismutase (MnSOD) activity. This compromised MnSOD activity is due to a significant increase in its level of glutathionylation. The incubation of hyperoxic macrophages with 3.3 μM of GAT107 significantly decreases the levels of glutathionylated MnSOD and restores MnSOD activity and mitochondrial membrane integrity. Thus, GAT107 restored hyperoxia-compromised phagocytic functions by decreasing HMGB1 release, most likely via a mitochondrial-directed pathway.[1]
In vivo GAT107 (3.3 mg/kg; i.p.) significantly decreased animal mortality and markers of inflammatory injury in mice exposed to hyperoxia and subsequently infected with Pseudomonas aeruginosa.[1]
Synonyms GAT 107, GAT-107
Molecular Weight 405.31
Formula C18H17BrN2O2S
CAS No. 1476807-74-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45 mg/mL (111.03 mM)

TargetMolReferences and Literature

1. Gauthier AG, et al. GAT107-mediated α7 nicotinic acetylcholine receptor signaling attenuates inflammatory lung injury and mortality in a mouse model of ventilator-associated pneumonia by alleviating macrophage mitochondrial oxidative stress via reducing MnSOD-S-glutathionylation. Redox Biol. 2023 Apr;60:102614. 2. Papke RL, et al. The activity of GAT107, an allosteric activator and positive modulator of α7 nicotinic acetylcholine receptors (nAChR), is regulated by aromatic amino acids that span the subunit interface. J Biol Chem. 2014 Feb 14;289(7):4515-31. 3. Brems BM, et al. Dose-dependent effects of GAT107, a novel allosteric agonist-positive allosteric modulator (ago-PAM) for the α7 nicotinic cholinergic receptor: a BOLD phMRI and connectivity study on awake rats. Front Neurosci. 2023 Jun 23;17:1196786. 4. Gauthier AG, et al. The Positive Allosteric Modulation of alpha7-Nicotinic Cholinergic Receptors by GAT107 Increases Bacterial Lung Clearance in Hyperoxic Mice by Decreasing Oxidative Stress in Macrophages. Antioxidants (Basel). 2021 Jan 19;10(1):135.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library Membrane Protein-targeted Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

GAT107 1476807-74-5 Neuroscience AChR GAT 107 GAT-107 inhibitor inhibit

 

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