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Description: TrkB receptor antagonist
Chemical Name: N-[2-[[(Hexahydro-2-oxo-1H-azepin-3-yl)amino]carbonyl]phenyl]benzo[b]thiophene-2-carboxamide
Purity: ≥98% (HPLC)
Biological Activity for ANA 12
ANA 12 is a 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 for ANA 12
ANA 12 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for ANA 12
| M. Wt | 407.49 |
| Formula | C22H21N3O3S |
| Storage | Store at +4°C |
| Purity | ≥98% (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 for ANA 12
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 8.15 | 20 |
Preparing Stock Solutions for ANA 12
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 for ANA 12
References for ANA 12
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
If you know of a relevant reference for ANA 12, please let us know.
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Keywords: ANA 12, ANA 12 supplier, ANA12, TrkB, receptors, antagonists, BDNF, antidepressants, antagonisms, anti-seizure, KCC2, epilepsy, depression, Trk, Receptors, 4781, Tocris Bioscience
14 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
Marisela et al (2021) Cleaved PINK1 induces neuronal plasticity through PKA-mediated BDNF functional regulation. J Neurosci Res 99 2134-2155 PMID: 34046942
Zhou et al (2019) Microglia Are Indispensable for Synaptic Plasticity in the Spinal Dorsal Horn and Chronic Pain. Cell Rep 27 3844 PMID: 31242418
Livingstone et al (2019) Secreted Amyloid Precursor Protein-Alpha Promotes Arc Protein Synthesis in Hippocampal Neurons. Front Mol Neurosci 12 198 PMID: 31474829
Bernhard et al (2018) Parvalbumin-Interneuron Output Synapses Show Spike-Timing-Dependent Plasticity that Contributes to Auditory Map Remodeling. Neuron 99 720-735.e6 PMID: 30078579
Hang et al (2018) Minocycline promotes posthemorrhagic neurogenesis via M2 microglia polarization via upregulation of the TrkB/BDNF pathway in rats. J Neurophysiol 120 1307-1317 PMID: 29790836
Vicente et al (2022) Enhanced BDNF and TrkB Activation Enhance GABA Neurotransmission in Cerebellum in Hyperammonemia. Int J Mol Sci 23 PMID: 36233065
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
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
Jun et al (2020) Prolonged Use of NMDAR Antagonist Develops Analgesic Tolerance in Neuropathic Pain via Nitric Oxide Reduction-Induced GABAergic Disinhibition. Neurotherapeutics 17 1016-1030 PMID: 32632774
Nury et al (2020) Dynamic Fas signaling network regulates neural stem cell proliferation and memory enhancement. Sci Adv 6 eaaz9691 PMID: 32494656
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
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
Do you know of a great paper that uses ANA 12 from Tocris? Please let us know.
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Literature in this Area
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