GTS-21 dihydrochloride
Based on 14 publication(s) in Google Scholar
GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti inflammatory and cognition enhancing activities. GTS-21 dihydrochloride is also a α4β2 (Ki=20 nM for humanα4β2) and 5-HT3A receptor (IC50=3.1 μM) antagonist.
For research use only. We do not sell to patients.
- Purity: 99.65%
- CAS No.: 156223-05-1
- Formula: C19H22Cl2N2O2
- Molecular Weight:381.30
-
Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
GPCR/G Protein Compound Library
HY-L006
-
Immunology/Inflammation Compound Library
HY-L007
-
Membrane Transporter/Ion Channel Compound Library
HY-L011
-
Neuronal Signaling Compound Library
HY-L013
-
Clinical Compound Library
HY-L026
-
CNS-Penetrant Compound Library
HY-L028
-
Drug Repurposing Compound Library
HY-L035
-
Anti-COVID-19 Compound Library
HY-L052
-
Neurotransmitter Receptor Compound Library
HY-L062
-
Anti-Alzheimer's Disease Compound Library
HY-L069
-
Anti-Parkinson's Disease Compound Library
HY-L085
-
Neurodegenerative Disease-related Compound Library
HY-L086
-
5-HT Receptor Compound Library
HY-L121
-
Coagulation and Anti-coagulation Compound Library
HY-L136
-
Heterocyclic Compound Library
HY-L138
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Highly Selective Inhibitors Library
HY-L158
-
Highly Selective Activators Library
HY-L159
-
Ion Channel Compound Library
HY-L166
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
RNA Binding Bioactive Compound Library
HY-L248
-
Lactylation Compound Library
HY-L249
Publications Citing Use of MedChemExpress (MCE) GTS-21 dihydrochloride
More- Diabetologia. 2025 Dec 15. [Abstract]
- Biomed Pharmacother. 2022 May:149:112733. [Abstract]
- Cell Death Discov. 2022 Feb 8;8(1):54. [Abstract]
- Cell Death Discov. 2021 Mar 29;7(1):63. [Abstract]
- Diabetes Obes Metab. 2022 Jul;24(7):1255-1266. [Abstract]
- Front Pharmacol. 2021 Mar 17:12:593682. [Abstract]
- Int Immunopharmacol. 2024 Mar 10:129:111603. [Abstract]
- Mediators Inflamm. 2026 Jan 21:2026:4652344. [Abstract]
- Exp Neurol. 2025 Nov 19:397:115562. [Abstract]
- Mediators Inflamm. 2020 Sep 29:2020:1320278. [Abstract]
- Neurosci Lett. 2023 Jan 18:794:136995. [Abstract]
- SSRN. 2023 Jul 25.
- Research Square Preprint. 2023 May 30.
- Research Square Preprint. 2021 Jul.
Customer Validation & Images
-
WB
-
Flow Cytometry
-
Cell Imaging/Staining
-
WB
-
WB
All 5-HT Receptor Isoforms
More
Biological Activity
|
5-HT3A Receptor |
α7-nAChR |
human α4β2 20 nM (Ki) |
5-HT3A Receptor 3.1 μM (IC50) |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL6 mice were irradiated with 12 Gy to induce a mouse model of Radiation induced lung injury (RILI)[3]
-
Dosage:4 mg/kg
-
Administration:I.p.; 1, 3, 7, 14 and 21 days
-
Result:Reduces lung inflammatory infiltrate and fibrosis in radiation treated mice.
Chemical Information
-
CAS No. 156223-05-1
-
Appearance Solid
-
Molecular Weight 381.30
-
Formula C19H22Cl2N2O2
-
Color Light yellow to yellow
-
SMILES
COC1=CC(OC)=CC=C1/C=C2CCCN=C\2C3=CC=CN=C3.Cl[H].Cl[H]
-
Synonyms
DMXB-A; DMBX-anabaseine
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (14)
-
Journal Impact Factor
-
Most Recent
-
Diabetologia
α7 Nicotinic acetylcholine receptor activation rescues mitochondrial dysfunction in gestational diabetes mellitus by competing with p66Shc for VDAC1 binding. [Abstract]2025 Dec 15. PMID: 41396300
GTS-21 dihydrochloride purchased from MedChemExpress. Usage Cited in: Diabetologia. 2025 Dec 15. [Abstract]
HTR8/SVneo cells were treated with nicotine (NT), PNU or GTS-21 dihydrochloride (1 μM) at different concentrations (0, 0.1, 1, 10 μM) for 24 h under HG. Western blot images and quantification of p-p66Shc and p21 relative to GAPDH.
GTS-21 dihydrochloride purchased from MedChemExpress. Usage Cited in: Diabetologia. 2025 Dec 15. [Abstract]
HTR8/SVneo cells or primary feeder cells were treated with normal glucose (NG), high glucose (HG), high glucose + PNU, or high glucose + GTS-21 dihydrochloride (1 μM), respectively. Mitochondrial membrane potential (MMP) was analyzed by flow cytometry using JC-1 staining.
GTS-21 dihydrochloride purchased from MedChemExpress. Usage Cited in: Diabetologia. 2025 Dec 15. [Abstract]
HTR8/SVneo cells or primary trophoblast cells were treated with normal glucose (NG), high glucose (HG), high glucose + PNU, or high glucose + GTS-21 dihydrochloride (1 μM), respectively. Representative confocal microscopy images of mitochondrial permeability transition pore (mPTP) opening experiments quenched with calcein AM (green) and cobalt chloride (CoCl₂).
-
Biomed Pharmacother
Activation of α7nAChR preserves intestinal barrier integrity by enhancing the HO-1 / STAT3 signaling to inhibit NF-κB activation in mice. [Abstract]2022 May:149:112733. PMID: 36068769
GTS-21 dihydrochloride purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2022 May:149:112733. [Abstract]
GTS-21 dihydrochloride (10 μM). The relative expression levels of ZO-1, Occludin, and Claudin-1 in Caco2 cells were analyzed by Western blot.
-
Cell Death Discov
Vagus nerve stimulation alleviated cerebral ischemia and reperfusion injury in rats by inhibiting pyroptosis via α7 nicotinic acetylcholine receptor. [Abstract]2022 Feb 8;8(1):54. PMID: 35136042
GTS-21 dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2022 Feb 8;8(1):54. [Abstract]
Intraperitoneal injection of GTS-21 (4 mg/kg) significantly downregulated the expression of NLRP3, ASC, Cl-Caspase-1 and GSDMD-N.
-
Cell Death Discov
Vagus nerve stimulation enhances the cholinergic anti-inflammatory pathway to reduce lung injury in acute respiratory distress syndrome via STAT3. [Abstract]2021 Mar 29;7(1):63. PMID: 33782389 -
Diabetes Obes Metab
The alpha-7 nicotinic acetylcholine receptor agonist GTS-21 engages the glucagon-like peptide-1 incretin hormone axis to lower levels of blood glucose in db/db mice. [Abstract]2022 Jul;24(7):1255-1266. PMID: 35293666 -
Front Pharmacol
Activation of the Cholinergic Anti-inflammatory Pathway Attenuated Angiotension II-Dependent Hypertension and Renal Injury. [Abstract]2021 Mar 17:12:593682. PMID: 33815099 -
Int Immunopharmacol
GTS-21 attenuates ACE/ACE2 ratio and glycocalyx shedding in lipopolysaccharide-induced acute lung injury by targeting macrophage polarization derived ADAM-17. [Abstract]2024 Mar 10:129:111603. PMID: 38310766 -
Mediators Inflamm
Nicotine Regulates LPS-Induced Inflammatory Responses in HMC3 Microglia and Exerts Neuronal Protection. [Abstract]2026 Jan 21:2026:4652344. PMID: 41583120 -
Exp Neurol
Alpha 7 nicotinic acetylcholine receptor contributes to long-term cognitive recovery following ischemic stroke. [Abstract]2025 Nov 19:397:115562. PMID: 41270982 -
Mediators Inflamm
Exploring the Mechanism on the Medullary Visceral Zone Inhibiting the Cholinergic Anti-inflammatory Pathway Induced by Sepsis. [Abstract]2020 Sep 29:2020:1320278. PMID: 33061821 -
Neurosci Lett
Inhibiting specificity protein 1 attenuated sevoflurane-induced mitochondrial stress and promoted autophagy in hippocampal neurons through PI3K/Akt/mTOR and α7-nAChR signaling. [Abstract]2023 Jan 18:794:136995. PMID: 36464148 -
-
-
Solvent & Solubility
H2O : 50 mg/mL (131.13 mM; Need ultrasonic)
DMSO : 16.5 mg/mL (43.27 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Add each solvent one by one: PBS
Solubility: 75 mg/mL (196.70 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
-
Data Sheet (280 KB)
-
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Portuguese - PT (254 KB)
-
Handling Instructions (2659 KB)
References
[1]. Briggs CA, et al. Functional characterization of the novel neuronal nicotinic acetylcholine receptor ligand GTS-21 in vitro and in vivo. Pharmacol Biochem Behav. 1997;57(1-2):231-241. [Content Brief]
[2]. Zhang R, et al. N-terminal domains in mouse and human 5-hydroxytryptamine3A receptors confer partial agonist and antagonist properties to benzylidene analogs of anabaseine. J Pharmacol Exp Ther. 2006;317(3):1276-1284. [Content Brief]
[3]. Mei Z, et al. α7 nAchR agonist GTS 21 reduces radiation induced lung injury. Oncol Rep. 2018;40(4):2287-2297. [Content Brief]
Complete Stock Solution Preparation Table
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 2.6226 mL | 13.1130 mL | 26.2261 mL | 65.5652 mL |
| 5 mM | 0.5245 mL | 2.6226 mL | 5.2452 mL | 13.1130 mL | |
| 10 mM | 0.2623 mL | 1.3113 mL | 2.6226 mL | 6.5565 mL | |
| 15 mM | 0.1748 mL | 0.8742 mL | 1.7484 mL | 4.3710 mL | |
| 20 mM | 0.1311 mL | 0.6557 mL | 1.3113 mL | 3.2783 mL | |
| 25 mM | 0.1049 mL | 0.5245 mL | 1.0490 mL | 2.6226 mL | |
| 30 mM | 0.0874 mL | 0.4371 mL | 0.8742 mL | 2.1855 mL | |
| 40 mM | 0.0656 mL | 0.3278 mL | 0.6557 mL | 1.6391 mL | |
| H2O | 50 mM | 0.0525 mL | 0.2623 mL | 0.5245 mL | 1.3113 mL |
| 60 mM | 0.0437 mL | 0.2186 mL | 0.4371 mL | 1.0928 mL | |
| 80 mM | 0.0328 mL | 0.1639 mL | 0.3278 mL | 0.8196 mL | |
| 100 mM | 0.0262 mL | 0.1311 mL | 0.2623 mL | 0.6557 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Powered by Bioz