ANA 12; ANA-12; ANA12
| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
Purity: ≥98%
ANA-12 (ANA12) is a novel, potent and selective TrkB inhibitor/antagonist with important biological activity. It has a Kd of 10 nM for the high affinity site of TrkB and 12 μM for the low affinity site.
| Targets |
TrkB (Kd = 10 nM)
|
|
|---|---|---|
| ln Vitro |
|
|
| ln Vivo |
|
|
| Enzyme Assay |
Various concentrations of Trk BECD -Fc, 20 mg/ml BSA, or 1 mg/mL IgG-Fc (polyclonal anti-TrkB) are coated on Maxisorp ELISA 96-well plates and left overnight at 4°C in a carbonate buffer with a pH of 9.6. After two hours of room temperature solubility in 0.5% BSA in PBS, plates are thoroughly cleaned in PBS-Tween 0.05%. Following an hour of room temperature incubation in 0.5% PBS-BSA, BDNF is added to the solution and incubated for an additional hour. This process is repeated with Bodipy-ANA-12. The amount of bodipy-ANA-12 bound is measured by fluorescence at 520 ± 10 nm following thorough washes in PBS-Tween 0.05%. To determine the detectability range for extrapolation analysis, ELISA plates are coated with bodipy-ANA-12, and the fluorescence at 520 ± 10 nm is measured.
|
|
| Cell Assay |
In nnr5 PC12-TrkB, -TrkA, and -TrkC cells, the effects of molecules on neurite outgrowth are evaluated following the addition of BDNF (1 nM), NGF (2 nM), and NT-3 (10 nM), respectively. A microscope counts the number of cells in each counting field—three wells per condition, two fields per well—that have neurites longer than two cells in diameter. For three days, the counting is done in the dark every 24 hours.
|
|
| Animal Protocol |
In a vehicle of 17% dimethyl sulfoxide (DMSO) in phosphate-buffered saline, ketamine (ketamine hydrochloride, 10 mg/kg), 7,8-dihydroxyflavone (7,8-DHF; 10 mg/kg), and ANA-12, N2-(2-{[(2-oxoazepan-3-yl) amino]carbonyl}phenyl)benzo[b]thiophene-2-carboxamide (0.5 mg/kg) are prepared on the day of injection. Ketamine (10 mg/kg), 7,8-DHF (10 mg/kg), and ANA-12 (0.5 mg/kg) are the doses that have been chosen. Mice receive intraperitoneal (i.p.) administration of all compounds.
|
|
| References |
| Molecular Formula |
C22H21N3O3S
|
|
|---|---|---|
| Molecular Weight |
407.49
|
|
| Exact Mass |
407.13
|
|
| Elemental Analysis |
C, 64.85; H, 5.19; N, 10.31; O, 11.78; S, 7.87
|
|
| CAS # |
219766-25-3
|
|
| Related CAS # |
|
|
| Appearance |
Solid powder
|
|
| SMILES |
C1CCNC(=O)C(C1)NC(=O)C2=CC=CC=C2NC(=O)C3=CC4=CC=CC=C4S3
|
|
| InChi Key |
TUSCYCAIGRVBMD-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C22H21N3O3S/c26-20(25-17-10-5-6-12-23-21(17)27)15-8-2-3-9-16(15)24-22(28)19-13-14-7-1-4-11-18(14)29-19/h1-4,7-9,11,13,17H,5-6,10,12H2,(H,23,27)(H,24,28)(H,25,26)
|
|
| Chemical Name |
N-[2-[(2-oxoazepan-3-yl)carbamoyl]phenyl]-1-benzothiophene-2-carboxamide
|
|
| Synonyms |
|
|
| HS Tariff Code |
2934.99.9001
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1.43 mg/mL (3.51 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.43 mg/mL (3.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 1 mg/mL (2.45 mM) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Solubility in Formulation 4: ≥ 0.45 mg/mL (1.10 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 5: ≥ 0.45 mg/mL (1.10 mM) (saturation unknown) in 5% DMSO + 95% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 6: 2% DMSO+30% PEG 300+2% Tween 80+ddH2O: 2mg/mL . |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4540 mL | 12.2702 mL | 24.5405 mL | |
| 5 mM | 0.4908 mL | 2.4540 mL | 4.9081 mL | |
| 10 mM | 0.2454 mL | 1.2270 mL | 2.4540 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Effects of 7,8-DHF and ANA-12 on LPS-induced changes in phosphorylation of TrkB in the mouse brain. Int J Neuropsychopharmacol. 2015 Feb; 18(4): pyu077. |
Role of TrkB and mTORC1 in the antidepressant action of 7,8-DHF and ANA-12 on LPS-induced depression-like behavior. Int J Neuropsychopharmacol. 2014 Oct 31;18(4). |
Role of TrkB and mTORC1 in the antidepressant action of 7,8-DHF and ANA-12 on LPS-induced depression-like behavior. Int J Neuropsychopharmacol. 2014 Oct 31;18(4). |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
