GTS-21
Based on 16 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. GTS-21 can be used in age-associated memory impairment (AAMI) and Alzheimer's disease research.
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- CAS No.: 148372-04-7
- Formule: C19H20N2O2
- Masse moléculaire:308.37
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Publications Citing Use of MedChemExpress (MCE) GTS-21
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]
- Clin Transl Med. 2026 Jul;16(7):e70726. [Abstract]
- Diabetes Obes Metab. 2022 Jul;24(7):1255-1266. [Abstract]
- Front Pharmacol. 2021 Mar 17:12:593682. [Abstract]
- Int Immunopharmacol. 2026 Aug 15:183:116879. [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.
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Activité biologique
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5-HT3A Receptor |
α7-nAChR |
human α4β2 |
5-HT3A Receptor 3.1 μM (IC50) |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 148372-04-7
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Masse moléculaire 308.37
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Formule C19H20N2O2
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SMILES
COC(C=C(C=C1)OC)=C1/C=C2C(C3=CN=CC=C3)=NCCC/2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (16)
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Journal Impact Factor
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Most Recent
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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).
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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.
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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.
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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 -
Clin Transl Med
α7nAChR agonist GTS-21 ameliorates sepsis-induced acute kidney injury via MEF2/PGC-1α/HO-1 axis in mice. [Abstract]2026 Jul;16(7):e70726. PMID: 42333777 -
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 -
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Pureté et documentation
Références
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GTS-21 Related Classifications
HY-14564 Related Classifications
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