ANA-12

Catalog No.S7745 Batch:S774502

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Technical Data

Formula

C22H21N3O3S
Molecular Weight 407.49 CAS No. 219766-25-3
Solubility (25°C)* In vitro DMSO 81 mg/mL (198.77 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
2%DMSO 30%PEG300 2%Tween80 66%ddH2O
2.0mg/ml Taking the 1 mL working solution as an example, add 20 μL of 100 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 660 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.)

Preparing Stock Solutions

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 29 publications

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
Utility of 7,8-dihydroxyflavone in preventing astrocytic and synaptic deficits in the hippocampus elicited by PTSD [ Pharmacol Res, 2022, 176:106079] PubMed: 35026406
lncRNA BDNF-AS Attenuates Propofol-Induced Apoptosis in HT22 Cells by Modulating the BDNF/TrkB Pathway [ Mol Neurobiol, 2022, 10.1007/s12035-022-02757-y] PubMed: 35338452
Reduced BDNF expression in the auditory cortex contributed to neonatal pain-induced hearing impairment and dendritic pruning deficiency in mice [ Reg Anesth Pain Med, 2022, rapm-2022-103621] PubMed: 36384877
Atorvastatin inhibits neuronal apoptosis via activating cAMP/PKA/p-CREB/BDNF pathway in hypoxic-ischemic neonatal rats [ FASEB J, 2022, 36(4):e22263] PubMed: 35303316
[ANA- 12 inhibits spinal inflammation and alleviates acute and chronic pain in rats by targeted blocking of BDNF/TrkB signaling] [ Nan Fang Yi Ke Da Xue Xue Bao, 2022, 42(2):232-237] PubMed: 35365447
Melatonin protects inner retinal neurons of newborn mice after hypoxia-ischemia [ J Pineal Res, 2021, 71(1):e12716] PubMed: 33426650
Striatal Shati/Nat8l-BDNF pathways determine the sensitivity to social defeat stress in mice through epigenetic regulation [ Neuropsychopharmacology, 2021, 10.1038/s41386-021-01033-2] PubMed: 34099867
Striatal Shati/Nat8l-BDNF pathways determine the sensitivity to social defeat stress in mice through epigenetic regulation [ Neuropsychopharmacology, 2021, 46(9):1594-1605] PubMed: 34099867

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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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.