ANA 12

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Cat.No. 4781 - ANA 12 | C22H21N3O3S | CAS No. 219766-25-3
Description: TrkB receptor antagonist
Chemical Name: N-[2-[[(Hexahydro-2-oxo-1H-azepin-3-yl)amino]carbonyl]phenyl]benzo[b]thiophene-2-carboxamide
Purity: ≥99% (HPLC)
Datasheet
Citations (8)
Reviews
Literature (6)

Biological Activity

TrkB receptor antagonist. Demonstrates a 2-site mode of action, preventing activation by BDNF non-competitively (IC50 values are 45.6 nM and 41.1 μM for the high and low affinity sites respectively). Displays no effect on TrkA and TrkC in an assay of neurite outgrowth. Demonstrates antidepressant properties. Also exhibits anti-seizure effects in an ischemia-induced neonatal seizure model by blocking down-regulation of KCC2.

Compound Libraries

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Technical Data

M. Wt 407.49
Formula C22H21N3O3S
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 219766-25-3
PubChem ID 2799722
InChI Key TUSCYCAIGRVBMD-UHFFFAOYSA-N
Smiles O=C(NC4C(NCCCC4)=O)C1=C(NC(C2=CC3=C(C=CC=C3)S2)=O)C=CC=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 8.15 20

Preparing Stock Solutions

The following data is based on the product molecular weight 407.49. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.2 mM 12.27 mL 61.35 mL 122.7 mL
1 mM 2.45 mL 12.27 mL 24.54 mL
2 mM 1.23 mL 6.14 mL 12.27 mL
10 mM 0.25 mL 1.23 mL 2.45 mL

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Product Datasheets

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References

References are publications that support the biological activity of the product.

Cazorla et al (2011) Identification of a low-molecular weight TrkB antagonist with anxiolytic and antidepressant activity in mice. J.Clin.Invest. 121 1846 PMID: 21505263

Carter et al (2018) Dose-dependent reversal of KCC2 hypofunction and phenobarbital-resistant neonatal seizures by ANA12. Sci.Rep. 8 11987 PMID: 30097625


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View all Trk Receptor Antagonists

Keywords: ANA 12, ANA 12 supplier, ANA12, TrkB, receptors, antagonists, BDNF, antidepressants, antagonisms, anti-seizure, KCC2, Trk, Receptors, 4781, Tocris Bioscience

8 Citations for ANA 12

Citations are publications that use Tocris products. Selected citations for ANA 12 include:

Stepan et al (2015) High-Speed imaging reveals opposing effects of chronic stress and antidepressants on neuronal activity propagation through the hippocampal trisynaptic circuit. Front Neural Circuits 9 70 PMID: 26594153

Livingstone et al (2019) Secreted Amyloid Precursor Protein-Alpha Promotes Arc Protein Synthesis in Hippocampal Neurons. Front Mol Neurosci 12 198 PMID: 31474829

Zhou et al (2019) Microglia Are Indispensable for Synaptic Plasticity in the Spinal Dorsal Horn and Chronic Pain. Cell Rep 27 3844 PMID: 31242418

O'Neill et al (2018) The 3' UTRs of Brain-Derived Neurotrophic Factor Transcripts Differentially Regulate the Dendritic Arbor. Front Cell Neurosci 12 60 PMID: 29563866

Fischer et al (2017) Subthalamic Nucleus Deep Brain Stimulation Employs trkB Signaling for Neuroprotection and Functional Restoration. J Neurosci 37 6786 PMID: 28607168

Hashimotodani et al (2017) LTP at Hilar Mossy Cell-Dentate Granule Cell Synapses Modulates Dentate Gyrus Output by Increasing Excitation/Inhibition Balance. Neuron 95 928 PMID: 28817805

Han et al (2018) 7,8,3'-Trihydroxyflavone ameliorate oxidative stress in vivo and promotes neurite regeneration in vitro in rat retinal ganglion cells. Eur.J.Pharmacol. 823 283 PMID: 29886238

Shamblott et al (2016) Neurogenin 3 is regulated by neurotrophic tyrosine kinase receptor type 2(TRKB) signaling in the adult human exocrine pancreas. Cell Communication and Signaling 14 23 PMID: 27659207


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