ANA 12 |
| カタログ番号GC11486 |
ANA 12 は、強力かつ選択的な TrkB アンタゴニストであり、12 μM の Kd で TrkBECD-Fc に結合します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 219766-25-3
Sample solution is provided at 25 µL, 10mM.
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ANA 12 is a potent and selective antagonist of TrkB with IC50 values of 45.6 nM and 41.1 μM for the high and low affinity sites, respectively [1].
Tropomyosin-related kinase B (TrkB) is a receptor for brain-derived neurotrophic factor (BDNF) and neurotrophin-4/5 (NT-4/5) and activates 3 major signaling pathways involving phospholipase C-γ, PI3K and MAPK. The BDNF/TrkB signaling plays an important role in drug addiction, depression and anxiety [1].
ANA 12 is a potent and selective TrkB antagonist. ANA-12 bound to the extracellular low-affinity site of TrkB with Kd value of 12 μM in a dose-dependent way. And ANA-12 bound to the high-affinity site with Kd value of 10 nM. Also, ANA-12 bound to TrkB in a noncompetitive mechanism. In the TrkB-expressing cells, ANA-12 (10 nM) effectively inhibited BDNF-induced neurite outgrowth and completely abolished the effects of BDNF at 10-100 μM [1].
In the mice brain, ANA-12 (0.5 mg/kg) inhibited endogenous TrkB activity by 25% 4 hours later. Also, ANA-12 showed antidepressant and anxiolytic activities [1].
Reference:
[1]. Cazorla M, Prémont J, Mann A, et al. Identification of a low-molecular weight TrkB antagonist with anxiolytic and antidepressant activity in mice. J Clin Invest, 2011, 121(5): 1846-1857.
| Binding experiment [1]: | |
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Binding assays |
Maxisorp ELISA 96-well plates were coated with various concentrations of TrkBECD-Fc, 20 mg/ml BSA, or 1 mg/ml IgG-Fc in a carbonate buffer (pH 9.6) overnight at 4°C. Plates were saturated with 0.5% BSA in PBS for 2 hours at room temperature and extensively washed in PBS-Tween 0.05%. Bodipy–ANA-12 was 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 was quantified by fluorescence at 520 ± 10 nm. |
| Cell experiment [1]: | |
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Cell lines |
PC12-TrkB cell lines |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
0-100 μM for 3 days |
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Applications |
In the TrkB-expressing cells, ANA-12 prevented brain-derived neurotrophic factor-induced neurite outgrowth at concentrations as low as 10 nM. At concentrations up to 10–100 μM, ANA-12 completely abolished the effects of brain-derived neurotrophic factor, and no single neurite or branching could be observed. |
| Animal experiment [1]: | |
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Animal models |
Mice |
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Dosage form |
0.5 mg/kg |
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Application |
Mice administered ANA-12 demonstrated reduced anxiety- and depression-related behaviors on a variety of tests predictive of anxiolytic and antidepressant properties in humans. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Cazorla M, Prémont J, Mann A, et al. Identification of a low-molecular weight TrkB antagonist with anxiolytic and antidepressant activity in mice. J Clin Invest, 2011, 121(5): 1846-1857. | |
| Cas No. | 219766-25-3 | SDF | |
| Chemical Name | N-(2-((2-oxoazepan-3-yl)carbamoyl)phenyl)benzo[b]thiophene-2-carboxamide | ||
| Canonical SMILES | O=C(NC1CCCCNC1=O)C2=CC=CC=C2NC(C3=CC4=CC=CC=C4S3)=O | ||
| Formula | C22H21N3O3S | M.Wt | 407.49 |
| 溶解度 | ≥ 10.2mg/mL in DMSO with gentle warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.454 mL | 12.2702 mL | 24.5405 mL |
| 5 mM | 0.4908 mL | 2.454 mL | 4.9081 mL |
| 10 mM | 0.2454 mL | 1.227 mL | 2.454 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)
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