Cat. No.: HY-14564

GTS-21

15 Cited Publications

Customer Review

Based on 15 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 (K_i=20 nM for humanα4β2) and 5-HT3A receptor (IC₅₀=3.1 μM) antagonist. GTS-21 can be used in age-associated memory impairment (AAMI) and Alzheimer's disease research.

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

CAS No.: 148372-04-7
Formula: C₁₉H₂₀N₂O₂
Molecular Weight:308.37

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (276 KB)

GTS-21 Chemical Structure

CAS No.: 148372-04-7

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Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (15)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

5-HT_3A Receptor

α7-nAChR

human α4β2

5-HT_3A Receptor

3.1 μM (IC₅₀)

All 5-HT Receptor Isoforms :

In Vitro

GTS-21 bound to human α4β2 nAChR (K_i=20 nM) 100-fold more potently than to humanα7-nAChR, and is 18- and 2-fold less potent than (-)-nicotine at human α4β2 and a7 nAChR, respectively^[1].

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

In Vivo

GTS 21 (4 mg/kg; i.p.; 1, 3, 7, 14 and 21 days) reduces radiation induced histological signs of pulmonary injury^[3].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 148372-04-7
Molecular Weight 308.37
Formula C₁₉H₂₀N₂O₂
SMILES

COC(C=C(C=C1)OC)=C1/C=C2C(C3=CN=CC=C3)=NCCC/2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (15)

All WBFlow CytometryCell Imaging/Staining

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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 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 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 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 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 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

Electroacupuncture protects intestinal barrier integrity in MAFLD mice and is associated with a macrophage α7nAChR/exosomal miR-217-5p/epithelial HO-1 signaling axis. [Abstract]

2026 Aug 15:183:116879. PMID: 42161050
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
SSRN

2023 Jul 25.
Research Square Preprint

2023 May 30.
Research Square Preprint

2021 Jul.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 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]. 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]

Calculators

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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.

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GTS-21

Publications Citing Use of MedChemExpress (MCE) GTS-21

All 5-HT Receptor Isoforms