ANA 12

TrkB receptor antagonist CAS# 219766-25-3

ANA 12

Catalog No. BCC6287----Order now to get a substantial discount!

Product Name & Size Price Stock
ANA 12: 5mg $81 In Stock
ANA 12: 10mg Please Inquire In Stock
ANA 12: 20mg Please Inquire Please Inquire
ANA 12: 50mg Please Inquire Please Inquire
ANA 12: 100mg Please Inquire Please Inquire
ANA 12: 200mg Please Inquire Please Inquire
ANA 12: 500mg Please Inquire Please Inquire
ANA 12: 1000mg Please Inquire Please Inquire
Related Products

Quality Control of ANA 12

Number of papers citing our products

Chemical structure

ANA 12

3D structure

Chemical Properties of ANA 12

Cas No. 219766-25-3 SDF Download SDF
PubChem ID 2799722 Appearance Powder
Formula C22H21N3O3S M.Wt 407.49
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 9.09 mg/mL (22.31 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name N-[2-[(2-oxoazepan-3-yl)carbamoyl]phenyl]-1-benzothiophene-2-carboxamide
SMILES C1CCNC(=O)C(C1)NC(=O)C2=CC=CC=C2NC(=O)C3=CC4=CC=CC=C4S3
Standard InChIKey TUSCYCAIGRVBMD-UHFFFAOYSA-N
Standard InChI 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)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of ANA 12

DescriptionTrkB receptor antagonist. Demonstrates a 2-site mode of action, preventing activation by BDNF non-competitively (IC50 values are 45.6 nM and 41.1 μM for the high and low affinity sites respectively). Displays no effect on TrkA and TrkC in an assay of neurite outgrowth. Demonstrates antidepressant properties.

ANA 12 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

ANA 12 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of ANA 12

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.454 mL 12.2702 mL 24.5405 mL 49.081 mL 61.3512 mL
5 mM 0.4908 mL 2.454 mL 4.9081 mL 9.8162 mL 12.2702 mL
10 mM 0.2454 mL 1.227 mL 2.454 mL 4.9081 mL 6.1351 mL
50 mM 0.0491 mL 0.2454 mL 0.4908 mL 0.9816 mL 1.227 mL
100 mM 0.0245 mL 0.1227 mL 0.2454 mL 0.4908 mL 0.6135 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on ANA 12

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.

Featured Products
New Products
 

References on ANA 12

Comparison of ketamine, 7,8-dihydroxyflavone, and ANA-12 antidepressant effects in the social defeat stress model of depression.[Pubmed:26337614]

Psychopharmacology (Berl). 2015 Dec;232(23):4325-35.

RATIONALE: Brain-derived neurotrophic factor (BDNF) and signaling at its receptor, tropomyosin-related kinase B (TrkB), are implicated in the rapid and long-lasting antidepressant effects of ketamine. Moreover, a TrkB agonist, 7,8-dihydroxyflavone (7,8-DHF), and/or TrkB antagonist, ANA-12, shows antidepressant effects in animal models of depression. OBJECTIVE: The objective of this study is to compare the influence of ketamine, 7,8-DHF, and ANA-12 on antidepressant activity in the social defeat stress model. RESULTS: In the tail suspension and forced swimming tests, ketamine, 7,8-DHF, or ANA-12 markedly attenuated the increased immobility time in depressed mice compared with the vehicle-treated group. In the sucrose preference test, all drugs significantly improved the reduced preference in depressed mice at both 1 and 3 days after a single dose. Antidepressant effect of ketamine, but not 7,8-DHF or ANA-12, was still detectable 7 days after a single dose. Western blot analyses showed that ketamine, but not 7,8-DHF or ANA-12, markedly attenuated reduced levels of BDNF and postsynaptic density protein 95 (PSD-95) in the prefrontal cortex (PFC), dentate gyrus (DG), and CA3 of the hippocampus in depressed mice 8 days after a single dose. Furthermore, ketamine markedly increased reduced levels of GluA1 in the PFC and DG of depressed mice. In contrast, ketamine showed no effect against increased levels of BDNF, PSD-95, and GluA1 observed in the nucleus accumbens of depressed mice. CONCLUSIONS: Compared with 7,8-DHF and ANA-12, ketamine is a longer-lasting antidepressant in the social defeat stress model, and synaptogenesis may be required for the mechanisms that promote sustained antidepressant effects of ketamine.

Identification of a low-molecular weight TrkB antagonist with anxiolytic and antidepressant activity in mice.[Pubmed:21505263]

J Clin Invest. 2011 May;121(5):1846-57.

The neurotrophin brain-derived neurotrophic factor (BDNF) and its receptor tropomyosin-related kinase B (TrkB) have emerged as key mediators in the pathophysiology of several mood disorders, including anxiety and depression. However, therapeutic compounds that interact with TrkB receptors have been difficult to develop. Using a combination of structure-based in silico screening and high-capacity functional assays in recombinant and neuronal cells, we identified a low-molecular weight TrkB ligand (ANA-12) that prevented activation of the receptor by BDNF with a high potency. ANA-12 showed direct and selective binding to TrkB and inhibited processes downstream of TrkB without altering TrkA and TrkC functions. KIRA-ELISA analysis demonstrated that systemic administration of ANA-12 to adult mice decreased TrkB activity in the brain without affecting neuronal survival. Mice administered ANA-12 demonstrated reduced anxiety- and depression-related behaviors on a variety of tests predictive of anxiolytic and antidepressant properties in humans. This study demonstrates that structure-based virtual screening strategy can be an efficient method for discovering potent TrkB-selective ligands that are active in vivo. We further propose that ANA-12 may be a valuable tool for studying BDNF/TrkB signaling and may constitute a lead compound for developing the next generation of therapeutic agents for the treatment of mood disorders.

Description

ANA-12 is a potent and selective TrkB antagonist with IC50s of 45.6 nM and 41.1 μM for the high and low affinity sites, respectively.

Keywords:

ANA 12,219766-25-3,Natural Products,Trk, buy ANA 12 , ANA 12 supplier , purchase ANA 12 , ANA 12 cost , ANA 12 manufacturer , order ANA 12 , high purity ANA 12

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: