Cat. No.: HY-12497

ANA-12

39 Cited Publications

Customer Review

Based on 39 publication(s) in Google Scholar

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.

For research use only. We do not sell to patients.

Purity: 99.90%
CAS No.: 219766-25-3
Formula: C₂₂H₂₁N₃O₃S
Molecular Weight:407.49

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

ANA-12 Chemical Structure

CAS No.: 219766-25-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (39)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

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.

IC₅₀ & Target

TrkB

All Trk Receptor Isoforms :

In Vitro

ANA-12 (10 nM) prevents BDNF-induced neurite outgrowth in the TrkB-expressing cells, and completely abolishes the effects of BDNF at concentrations up to 10-100 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

ANA-12 (0.5 mg/kg, i.p.) partially inhibits the total endogenous TrkB activity in the whole brain of mice. ANA-12, injected in mice, demonstrates anxiolytic and antidepressive activities at 0.5 mg/kg. ANA-12 (0.5, 1.0, and 2.0 mg/kg) does not affect neuron survival^[1]. ANA-12 (0.5 mg/kg) shows antidepressant effects in lipopolysaccharide (LPS)-induced depression-like behavior. ANA-12 (0.5 mg/kg) significantly attenuates an increased immobility time in depressed mice. In the TST, FST, and SPT, ANA-12 (0.5 mg/kg) does not show antidepressant-like effects in the control mice^[2]. ANA-12 (0.5 mg/kg, i.p.) reverses the diminished self-administration of cocaine in CocSired rats^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 219766-25-3
Appearance Solid
Molecular Weight 407.49
Formula C₂₂H₂₁N₃O₃S
Color White to off-white
SMILES

O=C(C1=CC2=CC=CC=C2S1)NC3=CC=CC=C3C(NC4C(NCCCC4)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (39)

All WBIF

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Journal Impact Factor

Cell Metab

Cancer cells co-opt nociceptive nerves to thrive in nutrient-poor environments and upon nutrient-starvation therapies. [Abstract]

2022 Dec 6;34(12):1999-2017.e10. PMID: 36395769
Nat Commun

Mesenchymal stromal cells alleviate depressive and anxiety-like behaviors via a lung vagal-to-brain axis in male mice. [Abstract]

2023 Nov 16;14(1):7406. PMID: 37973914
Adv Sci (Weinh)

Hepatocyte BDNF Acts as a Novel Immune Checkpoint to Restrain TLR4-Mediated Acute Hepatitis. [Abstract]

2026 Mar 25:e21164. PMID: 41881032
J Neuroinflammation

Inhibition of P2X4R attenuates white matter injury in mice after intracerebral hemorrhage by regulating microglial phenotypes. [Abstract]

2021 Aug 23;18(1):184. PMID: 34425835

ANA-12 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2021 Aug 23;18(1):184. [Abstract]

ANA-12 (0.5 mg/kg/day, i.p., daily for 7 days, from 1 day before ICH) reversed the treatment effect of inhibition P2X4R on white matter injury after ICH.

ANA-12 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2021 Aug 23;18(1):184. [Abstract]

ANA-12 (0.5 mg/kg/day, i.p., daily for 7 days, from 1 day before ICH) reversed the treatment effect of inhibition P2X4R on white matter injury after ICH.
J Neuroinflammation

BDNF promotes activation of astrocytes and microglia contributing to neuroinflammation and mechanical allodynia in cyclophosphamide-induced cystitis. [Abstract]

2020 Jan 13;17(1):19. PMID: 31931832

ANA-12 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2020 Jan 13;17(1):19. [Abstract]

ANA-12 (0.5 mg/kg, i.p., every other day after CYP injection, from day 3 to day 9) restrained activation of astrocytes and microglia induced by CYP.
Phytomedicine

Xiaochaihutang ameliorates depression-like behaviors induced via chronic social defeat stress by regulating exon-specific Bdnf transcription through H3K18 acetylation in the hippocampus of mice. [Abstract]

2025 May:140:156567. PMID: 40068295
Phytomedicine

Astragaloside IV mediates radiation-induced neuronal damage through activation of BDNF-TrkB signaling. [Abstract]

2024 Jun 8:132:155803. PMID: 38876008
Biomed Pharmacother

Protective effects of 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside against cadmium toxicity involve BDNF/TrkB and PI3K/Akt signaling pathways. [Abstract]

2025 Oct 23:192:118602. PMID: 41135432
J Transl Med

Tumor microenvironment-preserving gliosarcoma organoids as an in vitro preclinical platform: a comparative analysis with glioblastoma models. [Abstract]

2025 Aug 14;23(1):915. PMID: 40813987
PLoS Biol

Mdga2 deficiency leads to an aberrant activation of BDNF/TrkB signaling that underlies autism-relevant synaptic and behavioral changes in mice. [Abstract]

2025 Apr 1;23(4):e3003047. PMID: 40168357
Neural Regen Res

Electroacupuncture treatment improves motor function and neurological outcomes after cerebral ischemia/reperfusion injury. [Abstract]

2022 Jul;17(7):1545-1555. PMID: 34916440
Phytother Res

Salidroside directly activates HSC70, revealing a new role for HSC70 in BDNF signalling and neurogenesis after cerebral ischemia. [Abstract]

2024 Jun;38(6):2619-2640. PMID: 38488455
Transl Psychiatry

The causal involvement of the BDNF-TrkB pathway in dentate gyrus in early-life stress-induced cognitive deficits in male mice. [Abstract]

2023 May 24;13(1):173. PMID: 37225683
Ecotoxicol Environ Saf

Amelioration of cholesterol sulfate for lead-induced CTX cell apoptosis based on BDNF signaling pathway mediated cholesterol metabolism. [Abstract]

2022 Dec 15:248:114307. PMID: 36423370
Neurosci Bull

Peripheral BDNF Regulates Somatosensory-Sympathetic Coupling in Brachial Plexus Avulsion-Induced Neuropathic Pain. [Abstract]

2023 Dec;39(12):1789-1806. PMID: 37335428
Chin Med

Electroacupuncture promotes BDNF-dependent neurogenesis via microglial reprogramming in a chronic stress model. [Abstract]

2026 Feb 3;21(1):62. PMID: 41634791
Cell Prolif

Flavonoid chrysin activates both TrkB and FGFR1 receptors while upregulates their endogenous ligands such as brain derived neurotrophic factor to promote human neurogenesis. [Abstract]

2025 Jan;58(1):e13732. PMID: 39331585
Drug Des Devel Ther

Edaravone Alleviated Propofol-Induced Neurotoxicity in Developing Hippocampus by mBDNF/TrkB/PI3K Pathway. [Abstract]

2021 Mar 30:15:1409-1422. PMID: 33833500
J Cell Mol Med

Engeletin alleviates depression-like phenotype by increasing synaptic plasticity via the BDNF-TrkB-mTORC1 signalling pathway. [Abstract]

2023 Dec;27(23):3928-3938. PMID: 37799103
J Ovarian Res

BDNF promotes mouse follicular development and reverses ovarian aging by promoting cell proliferation. [Abstract]

2023 Apr 27;16(1):83. PMID: 37106468
J Neurosci

A Time-Sensitive Plasticity Distinguishes the Rapid and Sustained Synaptic Actions of Ketamine from Its (2 R,6 R)-Hydroxynorketamine Metabolite. [Abstract]

2026 Feb 3:e0958252026. PMID: 41633835
ACS Pharmacol Transl Sci

Transient Stimulation with Psychoplastogens Is Sufficient to Initiate Neuronal Growth. [Abstract]

2020 Sep 11;4(2):452-460. PMID: 33860174
Eur Arch Psychiatry Clin Neurosci

Brain-derived neurotrophic factor-TrkB signaling in the medial prefrontal cortex plays a role in the anhedonia-like phenotype after spared nerve injury. [Abstract]

2020 Mar;270(2):195-205. PMID: 29882089
Mol Med Rep

Identification of genes and pathways associated with MDR in MCF-7/MDR breast cancer cells by RNA-seq analysis. [Abstract]

2018 May;17(5):6211-6226. PMID: 29512753
Front Neurosci

Tetramethylpyrazine Alleviates Behavioral and Psychological Symptoms of Dementia Through Facilitating Hippocampal Synaptic Plasticity in Rats With Chronic Cerebral Hypoperfusion. [Abstract]

2021 May 6:15:646537. PMID: 34025340
Neuroscience

Brain-derived neurotrophic factor in the ventrolateral orbital cortex regulates spared nerve injury-induced neuropathic pain and related emotional disorders in mice. [Abstract]

2025 Aug 20:584:250-263. PMID: 40846211
Brain Sci

The α-7 Nicotinic Receptor Positive Allosteric Modulator Alleviates Lipopolysaccharide Induced Depressive-like Behavior by Regulating Microglial Function, Trophic Factor, and Chloride Transporters in Mice. [Abstract]

2024 Mar 19;14(3):290. PMID: 38539677
Neuroscience

Sulforaphane Alleviates Lipopolysaccharide-induced Spatial Learning and Memory Dysfunction in Mice: The Role of BDNF-mTOR Signaling Pathway. [Abstract]

2018 Sep 15:388:357-366. PMID: 30086367

ANA-12 purchased from MedChemExpress. Usage Cited in: Neuroscience. 2018 Sep 15:388:357-366. [Abstract]

Effects of ANA-12 on inflammatory cytokines, synaptic proteins, BDNF-TrkB signaling pathways in mice treated with Sulforaphane (SFN) plus Lipopolysaccharide (LPS).
Exp Eye Res

Neurotrophin-4 as a promising therapy for corneal injuries: Enhancing epithelial repair and nerve regeneration in abrasion and alkali burn models. [Abstract]

2026 May:266:110917. PMID: 41679583
Exp Eye Res

Neuroprotective effects of methyl 3,4 dihydroxybenzoate in a mouse model of retinitis pigmentosa. [Abstract]

2017 Sep:162:86-96. PMID: 28709891

ANA-12 purchased from MedChemExpress. Usage Cited in: Exp Eye Res. 2017 Sep:162:86-96. [Abstract]

Blocking the BDNF pathway with ANA-12 prevents the protective effect of MDHB.
Tissue Cell

BDNF alleviates senescence and enhances osteogenic differentiation in bone marrow mesenchymal stem cells via the TrkB/PI3K/AKT pathway. [Abstract]

2025 May 9:96:102972. PMID: 40367890
Behav Brain Res

Sigma-1 receptor agonist PRE-084 increases BDNF by activating the ERK/CREB pathway to rescue learning and memory impairment caused by type II diabetes. [Abstract]

2025 Apr 27:484:115493. PMID: 39986614
Exp Ther Med

The activation of BDNF reduced inflammation in a spinal cord injury model by TrkB/p38 MAPK signaling. [Abstract]

2019 Mar;17(3):1688-1696. PMID: 30783437
Biochem Biophys Res Commun

Cordycepin buffers anisomycin-induced fear memory deficit by restoring hippocampal BDNF. [Abstract]

2023 Jul 12:665:118-123. PMID: 37156049
J Neurophysiol

cAMP-dependent protein kinase signaling is required for ( 2R,6R)-hydroxynorketamine to potentiate hippocampal glutamatergic transmission. [Abstract]

2024 Jan 1;131(1):64-74. PMID: 38050689
Sleep Breath

7,8-Dihydroxyflavone protects retinal ganglion cells against chronic intermittent hypoxia-induced oxidative stress damage via activation of the BDNF/TrkB signaling pathway. [Abstract]

2022 Mar;26(1):287-295. PMID: 33993395
Neurosci Lett

P2X4 receptor in the dorsal horn contributes to BDNF/TrkB and AMPA receptor activation in the pathogenesis of remifentanil-induced postoperative hyperalgesia in rats. [Abstract]

2021 Apr 17:750:135773. PMID: 33639220
Research Square Print

November 21st, 2022.
Patent

US20200030309A1

Solvent & Solubility

In Vitro:

DMSO : 7.69 mg/mL (18.87 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 1.43 mg/mL (3.51 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1.43 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.43 mg/mL (3.51 mM); Clear solution

This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 3

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: 1 mg/mL (2.45 mM); Suspended solution; Need ultrasonic

Protocol 4

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 0.45 mg/mL (1.10 mM); Clear solution

Protocol 5

Add each solvent one by one: 5% DMSO 95% Corn Oil

Solubility: ≥ 0.45 mg/mL (1.10 mM); Clear solution

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 2 mg/mL (4.91 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Animal Administration^[2]

On the day of injection, 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 in vehicle of 17 % dimethyl sulfoxide (DMSO) in phosphate-buffered saline. The doses of ketamine (10 mg/kg), 7,8-DHF (10 mg/kg), and ANA-12 (0.5 mg/kg) are selected. All compounds are administered intraperitoneally (i.p.) to mice.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Cazorla M, et al. Identification of a low-molecular weight TrkB antagonist with anxiolytic and antidepressant activity in mice. J Clin Invest. 2011 May;121(5):1846-57. [Content Brief]

[2]. Fang X, et al. Brain-derived neurotrophic factor-TrkB signaling in the medial prefrontal cortex plays a role in the anhedonia-like phenotype after spared nerve injury. Eur Arch Psychiatry Clin Neurosci. 2018 Jun 7. [Content Brief]

[3]. Zhang JC, et al. Comparison of ketamine, 7,8-dihydroxyflavone, and ANA-12 antidepressant effects in the social defeat stress model of depression. Psychopharmacology (Berl). 2015 Dec;232(23):4325-35. [Content Brief]

[4]. Vassoler FM, et al. Epigenetic inheritance of a cocaine-resistance phenotype. Nat Neurosci. 2013 Jan;16(1):42-7. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4540 mL	12.2702 mL	24.5405 mL	61.3512 mL
	5 mM	0.4908 mL	2.4540 mL	4.9081 mL	12.2702 mL
	10 mM	0.2454 mL	1.2270 mL	2.4540 mL	6.1351 mL
	15 mM	0.1636 mL	0.8180 mL	1.6360 mL	4.0901 mL

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ANA-12

Kinase Inhibitor Library

Neuronal Signaling Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Human Metabolite Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) ANA-12

All Trk Receptor Isoforms

Biological Activity

Chemical Information

Publications (39)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

ANA-12

Kinase Inhibitor Library

Neuronal Signaling Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Human Metabolite Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) ANA-12

All Trk Receptor Isoforms

Biological Activity

Chemical Information

Publications (39)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

ANA-12 Related Classifications

Cat. No.: HY-12497