Home Protein Tyrosine Kinase Trk receptor antagonist ANA-12 For research use only.

ANA-12

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

ANA-12 Chemical Structure

ANA-12 Chemical Structure

CAS No. 219766-25-3

Purity & Quality Control

ANA-12 Related Products

Signaling Pathway

Trk receptor Signaling Pathways

Trk receptor Signaling Pathway

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
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]
Kinase Assay 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 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot MMP-9 p-AKT / AKT 29861866
In Vivo
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]
Animal Research Animal Models Adult C57BL6/129SveV F1s mice
Dosages 0.5 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 407.49 Formula

C22H21N3O3S
CAS No. 219766-25-3 SDF Download ANA-12 SDF
Smiles C1CCNC(=O)C(C1)NC(=O)C2=CC=CC=C2NC(=O)C3=CC4=CC=CC=C4S3
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 37 mg/mL ( (90.79 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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.

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