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ANA 12 TrkB receptor antagonist

Catalog No.B5712
Size Price Stock Qty
10mM (in 1mL DMSO)
$90.00
In stock
5mg
$70.00
In stock
25mg
$210.00
In stock
100mg
$560.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Zhao J, Du J, et al. "Activation of cardiac TrkB receptor by its small molecular agonist 7,8-dihydroxyflavone inhibits doxorubicin-induced cardiotoxicity via enhancing mitochondrial oxidative phosphorylation." Free Radic Biol Med. 2019 Jan;130:557-567. PMID:30472367

Quality Control

Chemical structure

ANA 12

Related Biological Data

ANA 12

Protocol

Binding experiment [1]:

Binding assays

Maxisorp ELISA 96-well plates were coated with various concentrations of TrkBECD-Fc, 20 mg/ml BSA, or 1 mg/ml IgG-Fc in a carbonate buffer (pH 9.6) overnight at 4°C. Plates were saturated with 0.5% BSA in PBS for 2 hours at room temperature and extensively washed in PBS-Tween 0.05%. Bodipy–ANA-12 was then incubated in 0.5% PBS-BSA for 1 hour at room temperature before the addition of BDNF in 0.5% PBS-BSA for another hour. After extensive washes in PBS-Tween 0.05%, the amount of bodipy–ANA-12 bound was quantified by fluorescence at 520 ± 10 nm.

Cell experiment [1]:

Cell lines

PC12-TrkB cell lines

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0-100 μM for 3 days

Applications

In the TrkB-expressing cells, ANA-12 prevented brain-derived neurotrophic factor-induced neurite outgrowth at concentrations as low as 10 nM. At concentrations up to 10–100 μM, ANA-12 completely abolished the effects of brain-derived neurotrophic factor, and no single neurite or branching could be observed.

Animal experiment [1]:

Animal models

Mice

Dosage form

0.5 mg/kg

Application

Mice administered ANA-12 demonstrated reduced anxiety- and depression-related behaviors on a variety of tests predictive of anxiolytic and antidepressant properties in humans.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Cazorla M, Prémont J, Mann A, et al. Identification of a low-molecular weight TrkB antagonist with anxiolytic and antidepressant activity in mice. J Clin Invest, 2011, 121(5): 1846-1857.

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Chemical Properties

Cas No. 219766-25-3 SDF Download SDF
Synonyms N/A
Chemical Name N-(2-((2-oxoazepan-3-yl)carbamoyl)phenyl)benzo[b]thiophene-2-carboxamide
Canonical SMILES O=C(NC1CCCCNC1=O)C2=CC=CC=C2NC(C3=CC4=CC=CC=C4S3)=O
Formula C22H21N3O3S M.Wt 407.49
Solubility ≥10.2mg/mL in DMSO with gentle warming Storage Store at -20°C
Physical Appearance A solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

ANA 12 is a potent and selective antagonist of TrkB with IC50 values of 45.6 nM and 41.1 μM for the high and low affinity sites, respectively [1].

Tropomyosin-related kinase B (TrkB) is a receptor for brain-derived neurotrophic factor (BDNF) and neurotrophin-4/5 (NT-4/5) and activates 3 major signaling pathways involving phospholipase C-γ, PI3K and MAPK. The BDNF/TrkB signaling plays an important role in drug addiction, depression and anxiety [1].

ANA 12 is a potent and selective TrkB antagonist. ANA-12 bound to the extracellular low-affinity site of TrkB with Kd value of 12 μM in a dose-dependent way. And ANA-12 bound to the high-affinity site with Kd value of 10 nM. Also, ANA-12 bound to TrkB in a noncompetitive mechanism. In the TrkB-expressing cells, ANA-12 (10 nM) effectively inhibited BDNF-induced neurite outgrowth and completely abolished the effects of BDNF at 10-100 μM [1].

In the mice brain, ANA-12 (0.5 mg/kg) inhibited endogenous TrkB activity by 25% 4 hours later. Also, ANA-12 showed antidepressant and anxiolytic activities [1].

Reference:
[1].  Cazorla M, Prémont J, Mann A, et al. Identification of a low-molecular weight TrkB antagonist with anxiolytic and antidepressant activity in mice. J Clin Invest, 2011, 121(5): 1846-1857.