Home Protein Tyrosine Kinase Trk receptor antagonist ANA-12

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ANA-12 Trk receptor antagonist

Cat.No.S7745

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 Trk receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 407.49

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Chemical Information, Storage & Stability

Molecular Weight 407.49 Formula

C22H21N3O3S

 Storage (From the date of receipt)
CAS No. 219766-25-3 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1CCNC(=O)C(C1)NC(=O)C2=CC=CC=C2NC(=O)C3=CC4=CC=CC=C4S3

Solubility

In vitro
Batch:

DMSO : 37 mg/mL (90.79 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
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, this compound prevents brain-derived neurotrophic factor (BDNF)-induced neurite outgrowth at concentrations as low as 10 nM. [1] In DRG neurons, this chemical 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–this compound bound is quantified by fluorescence at 520 ± 10 nm. Detectability range for extrapolation analysis is assessed by coating ELISA plates with bodipy–this chemical and reading fluorescence at 520 ± 10 nm.
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, this compound shows antidepressant-like effects on lipopolysaccharide-induced depression-like behavior. [3] In male Sprague-Dawley rats, this chemical blocks the effect of medial nucleus tractus solitarius (mNTS) BDNF on reducing food intake. [4] In male wild-type mice, it reverses ethanol intake and induces D3 receptor downregulation, but is ineffective in D3R-/- mice. [5] In male CocSired rats, this compound reverses the diminished self-administration of cocaine. [6]
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/22374757/
  • [5] https://pubmed.ncbi.nlm.nih.gov/24584330/
  • [6] https://pubmed.ncbi.nlm.nih.gov/23242310/

Applications

Methods Biomarkers Images PMID
Western blot MMP-9 p-AKT / AKT S7745-WB1 29861866

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Frequently Asked Questions

Question 1:
Can you test to see if there is a vehicle (<50% DMSO) that it can be dissolved as a clear solution for injection?

Answer:
S7745 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 this compound in DMSO first. It dissolves in DMSO not readily, so 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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