GTS-21
Based on 17 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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 148372-04-7
- Formel: C19H20N2O2
- Molecular Weight:308.37
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) GTS-21
More- Diabetologia. 2025 Dec 15. [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]
- Int Immunopharmacol. 2026 Oct 1:186:117098.
- Int Immunopharmacol. 2026 Aug 15:183:116879. [Abstract]
- Int Immunopharmacol. 2024 Mar 10:129:111603. [Abstract]
- Front Pharmacol. 2021 Mar 17:12:593682. [Abstract]
- Mediators Inflamm. 2026 Jan 21:2026:4652344. [Abstract]
- Mediators Inflamm. 2020 Sep 29:2020:1320278. [Abstract]
- Exp Neurol. 2026 Mar:397:115562. [Abstract]
- Neurosci Lett. 2023 Jan 18:794:136995. [Abstract]
- SSRN. 2023 Jul 25.
- Research Square Preprint. 2023 May 30.
- Biomed Pharmacother. 2022 May:149:112733. [Abstract]
- Research Square Preprint. 2021 Jul.
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Biologische Aktivität
Beschreibung
IC50 & Target
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5-HT3A Receptor |
α7-nAChR |
human α4β2 |
5-HT3A Receptor 3.1 μM (IC50) |
In Vitro
GTS-21 bound to human α4β2 nAChR (Ki=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. Further protocols information, click here.
In Vivo
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
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 148372-04-7
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Appearance Solid
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Molecular Weight 308.37
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Formel C19H20N2O2
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Color White to off-white
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SMILES
COC(C=C(C=C1)OC)=C1/C=C2C(C3=CN=CC=C3)=NCCC/2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (17)
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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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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 -
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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 -
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 -
Mediators Inflamm
Nicotine Regulates LPS-Induced Inflammatory Responses in HMC3 Microglia and Exerts Neuronal Protection. [Abstract]2026 Jan 21:2026:4652344. PMID: 41583120 -
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 -
Exp Neurol
Alpha 7 nicotinic acetylcholine receptor contributes to long-term cognitive recovery following ischemic stroke. [Abstract]2026 Mar:397:115562. PMID: 41270982 -
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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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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Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[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
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
GTS-21 Related Classifications
HY-14564 Related Classifications
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