ANA-12

For research use only.

Catalog No.S7745

21 publications

ANA-12 Chemical Structure

CAS No. 219766-25-3

ANA-12 is a selective TrkB antagonist with Kd of 10 nM and 12 μM for the high and low affinity sites, respectively.

Selleck's ANA-12 has been cited by 21 publications

Purity & Quality Control

Choose Selective Trk receptor Inhibitors

Biological Activity

Description ANA-12 is a selective TrkB antagonist with Kd of 10 nM and 12 μM for the high and low affinity sites, respectively.
Targets
TrkB [1]
10 nM(Kd)
In vitro

ANA-12 binds directly and selectively to TrkB and inhibits processes downstream of TrkB without altering TrkA and TrkC functions. In nnr5 PC12-TrkB cells, ANA-12 prevents brain-derived neurotrophic factor (BDNF)-induced neurite outgrowth at concentrations as low as 10 nM. [1] In DRG neurons, ANA-12 eliminates the effect of BDNF on increasing inward current. [2]

Assay
Methods Test Index PMID
Western blot
MMP-9; 

PubMed: 29861866     


The cells were cultured for 24 hours in the presence or absence of ANA-12 (5 μM) and the effect of ANA-12 on MMP-9 expression in these cells were examined by Western blot analysis.

p-AKT / AKT ; 

PubMed: 27659207     


Western blot analyses of signaling activity downstream of TRKB. Levels of active protein kinase B (p(S473)AKT) following treatment with ANA-12 and 78D compared to DMSO carrier control. 

29861866 27659207
In vivo In adult C57BL6/129SveV F1s mice, ANA-12 (0.5 mg/kg, i.p.) decreases TrKB activity in the brain and reduces the anxiety- and depression-related behaviors without affecting the neuron survival. [1] In male C57BL/6 mice, ANA-12 (0.5 mg/kg, i.p.) shows antidepressant-like effects on lipopolysaccharide-induced depression-like behavior. [3] In male Sprague-Dawley rats, ANA-12 (3 μg/dose) blocks the effect of medial nucleus tractus solitarius (mNTS) BDNF on reducing food intake. [4] In male wild-type mice, ANA-12 reverses ethanol intake and induces D3 receptor downregulation, but is ineffective in D3R-/- mice. [5] In male CocSired rats, ANA-12 (0.5 mg/kg, i.p.) reverses the diminished self-administration of cocaine. [6]

Protocol

Kinase Assay:

[1]

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ANA-12 Binding assay:

Maxisorp ELISA 96-well plates are coated with various concentrations of Trk BECD -Fc, 20 mg/ml BSA, or 1 mg/mL IgG-Fc (polyclonal anti-TrkB) in a carbonate buffer (pH 9.6) overnight at 4°C. Plates are saturated with 0.5% BSA in PBS for 2 hours at room temperature and extensively washed in PBS-Tween 0.05%. Bodipy–ANA-12 is 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 is quantified by fluorescence at 520 ± 10 nm. Detectability range for extrapolation analysis is assessed by coating ELISA plates with bodipy–ANA-12 and reading fluorescence at 520 ± 10 nm.
Cell Research:

[1]

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  • Cell lines: nnr5 PC12–TrkA, nnr5 PC12–TrkB, and nnr5 PC12–TrkC cells
  • Concentrations: ~100 μM
  • Incubation Time: ~3 days
  • Method:

    Modulation of neurite outgrowth by molecules is assessed in nnr5 PC12–TrkB, –TrkA, and –TrkC cells after addition of BDNF (1 nM), NGF (2 nM), and NT-3 (10 nM), respectively. The number of cells bearing neurites longer than 2 cells in diameter in each counting field is microscopically determined (2 fields per well, 3 wells per condition). Counting is performed blind each 24 hours for 3 days.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Adult C57BL6/129SveV F1s mice
  • Dosages: 0.5 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 37 mg/mL warmed (90.79 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
2mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 407.49
Formula

C22H21N3O3S

CAS No. 219766-25-3
Storage powder
in solvent
Synonyms N/A
Smiles C1CCNC(=O)C(C1)NC(=O)C2=CC=CC=C2NC(=O)C3=CC4=CC=CC=C4S3

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
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% DMSO % % Tween 80 % ddH2O
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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

  • Question 1:

    Can you test to see if there is a vehicle (<50% DMSO) that ANA-12 can be dissolved as a clear solution for injection?

  • Answer:

    S7745 ANA-12 can be dissolved in 20% DMSO/castor oil at 10 mg/ml, and in 40% DMSO/40% PEG 300/20% ddH2O at 10 mg/ml. They are both clear solution. please dissolve the compound in DMSO first. ANA-12 dissolves in DMSO not readily, please sonicate and warm it in water bath at about 45 degree. When it dissolves clearly, then add castor oil or PEG, then ddH2O.

Trk receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID