Overview
Cat #:
A-215
Lyophilized Powder yes
Source Synthetic
MW: 407.49
Purity: >98%
Effective concentration 100-200 µM.
Structure
Chemical name N-[2-[(2-oxoazepan-3-yl)carbamoyl]phenyl]-1-benzothiophene-2-carboxamide.
Molecular formula C22H21N3O3S.
CAS No.: 219766-25-3
PubChem CID 2799722
Activity ANA-12 is a selective TrkB antagonist, shown to bind directly and selectively to TrkB, preventing activation by BDNF and inhibiting processes downstream of TrkB, in a 2-site mode of action (IC50 values are 45.6 nM and 41.1 μM for the high and low affinity sites, respectively), without altering TrkA and TrkC functions. In adult mice ANA-12 decreases TrkB activity in the brain without affecting neuronal survival, and reduces anxiety and depression related behaviors1.
References-Activity
- Cazorla, M. et al. (2011) J. Clin. Invest. 121, 1846.
Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at +4°C.
Solubility Soluble in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Storage of solutions Up to four weeks at 4°C or three months at -20°C.
Our bioassay
Alomone Labs ANA-12 inhibits BDNF-induced ERK1/2 (p42/44 MAPK) phosphorylation in TrkB-expressing HEK 293 cells.Serum-deprived cells were stimulated with 1 ng/ml Recombinant human BDNF protein (#B-250) in the presence of 0 µM, 100 µM and 200 µM ANA-12 (#A-215). Cell proteins were resolved by SDS-PAGE and probed with anti-phospho-ERK1/2.
Scientific background
ANA-12 is a low molecular weight ligand that acts as a selective tropomyosin receptor kinase B (TrkB) antagonist. The compound shows direct binding to TrkB receptor and prevents its activation by BDNF with high potency, without altering TrkA and TrkC functions. The compound is considered to be a valuable tool for studying the BDNF-TrkB signaling pathway1,2.
A study indicated that administration of ANA-12 has successfully reduced anxiety and depression related behaviors tested in mice1.
TrkB receptor and BDNF are key mediators in the pathophysiology of several mood disorders, including drug addiction, anxiety and depression. They play an important role in the regulation of synaptic transmission and plasticity1.
Target TrkB receptor
Lyophilized Powder
For research purposes only, not for human use
Last Update: 03/01/2024
Specifications
Citations
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