ANA-12

Catalog No.S7745 Batch:S774501

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Technical Data

Formula

C22H21N3O3S
Molecular Weight 407.49 CAS No. 219766-25-3
Solubility (25°C)* In vitro DMSO 37 mg/mL (90.79 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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]
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 (from reference)

Kinase Assay:

[1]
  • 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 Assay:

[1]
  • 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.
Animal Study:

[1]
  • Animal Models

    Adult C57BL6/129SveV F1s mice

  • Dosages

    0.5 mg/kg

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , Front Cell Neurosci, 2018, doi:10.3389/fncel.2018.00122]

Data from [Data independently produced by , , Am J Physiol Heart Circ Physiol, 2018, doi:10.1152/ajpheart.00245.2018]

Data from [Data independently produced by , , Neuroscience, 2018, 390:151-159]

Selleck's ANA-12 has been cited by 37 publications

Progressive reduction of nuclear receptor Nr4a1 mediates age-dependent cognitive decline [ Alzheimers Dement, 2024, 10.1002/alz.13819] PubMed: 38605605
HDAC6-dependent deacetylation of NGF dictates its ubiquitination and maintains primordial follicle dormancy [ Theranostics, 2024, 14(6):2345-2366] PubMed: 38646645
A rare olive compound oleacein functions as a TrkB agonist and mitigates neuroinflammation both in vitro and in vivo [ Cell Commun Signal, 2024, 22(1):309] PubMed: 38835076
Phosphodiesterase 7 inhibitor reduces stress-induced behavioral and cytoarchitectural changes in C57BL/6J mice by activating the BDNF/TrkB pathway [ Front Pharmacol, 2024, 15:1411652] PubMed: 39092219
IGF-1 and Glucocorticoid Receptors Are Potential Target Proteins for the NGF-Mimic Effect of β-Cyclocitral from Lavandula angustifolia Mill. in PC12 Cells [ Int J Mol Sci, 2024, 25(18)9763] PubMed: 39337253
Activation of GPER1 by G1 prevents PTSD-like behaviors in mice: Illustrating the mechanisms from BDNF/TrkB to mitochondria and synaptic connection [ CNS Neurosci Ther, 2024, 30(7):e14855] PubMed: 38992889
The synergistic effects of anoikis-related genes and EMT-related genes in the prognostic prediction of Wilms tumor [ Front Mol Biosci, 2024, 11:1469775] PubMed: 39351154
Hepatic stellate cells maintain liver homeostasis through paracrine neurotrophin-3 signaling that induces hepatocyte proliferation [ Sci Signal, 2023, 16(787):eadf6696] PubMed: 37253090
Periplaneta Americana (L.) extract activates the ERK/CREB/BDNF pathway to promote post-stroke neuroregeneration and recovery of neurological functions in rats [ J Ethnopharmacol, 2023, 10.1016/j.jep.2023.117400] PubMed: 37952730
Effect of ginsenoside Rg1 on learning and memory ability of brain aging mice induced by D-galactose [ Chinese Journal of Tissue Engineering Research, 2023, (28): 4487-4493.] PubMed: none

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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