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Chemical Structure| 156223-05-1 Chemical Structure| 156223-05-1

Structure of GTS-21 2HCl
CAS No.: 156223-05-1

Chemical Structure| 156223-05-1

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GTS-21 2HCl is a selective α7 nicotinic acetylcholine receptor agonist, has recently been established as a promising treatment for inflammation.

Synonyms: DMXB-A; DMBX-anabaseine; GTS-21 (hydrochloride)

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Product Details of GTS-21 2HCl

CAS No. :156223-05-1
Formula : C19H22Cl2N2O2
M.W : 381.30
SMILES Code : COC1=CC=C(/C=C2C(C3=CC=CN=C3)=NCCC/2)C(OC)=C1.[H]Cl.[H]Cl
Synonyms :
DMXB-A; DMBX-anabaseine; GTS-21 (hydrochloride)
MDL No. :MFCD18910849

Safety of GTS-21 2HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
CD14+ monocytes in whole blood cultures 100 µmol L−1 4 hours GTS-21 significantly suppressed endotoxin-stimulated TNF production in whole blood cultures to a similar extent in both RA patients and healthy controls. J Intern Med. 2010 Jul;268(1):94-101

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Sprague-Dawley rats Renal ischemia-reperfusion injury model Intraperitoneal injection 10 mg/kg First dose administered 20 min before ischemia, repeated 6-8 hours later To evaluate the protective effects of GTS-21 on renal ischemia-reperfusion injury, results showed that GTS-21 significantly attenuated renal dysfunction, tubular necrosis, neutrophil infiltration, and TNF-α expression. Kidney Int. 2008 Jul;74(1):62-9
Mice Burn injury model Intraperitoneal injection 4 mg/kg Twice daily for 14 days GTS-21 ameliorated the spinal expression of cytokines/chemokines, inflammatory transducer-proteins, mitigated motor neuron loss (MNL), synaptic denervation, and decreased muscle wasting (MW) in tibialis (25%), gastrocnemius (15%), and soleus (20%) relative to untreated wild type BI mice. J Cachexia Sarcopenia Muscle. 2025 Apr;16(2):e13755
Mice Experimental autoimmune myocarditis model Oral 5 mg/kg Once daily for 21 days GTS-21 alleviates the immune response, regulates the proportion and function of CD4+ Treg and macrophages by activating the cholinergic anti-inflammatory pathway, and finally reduces heart inflammatory injury and improves cardiac remodeling. J Neuroinflammation. 2023 Apr 17;20(1):94
Mice LPS-induced lung injury model Intratracheal administration 4 mg/kg Single dose GTS-21 reversed the reduction of FGF10 expression in the lungs, as well as the number of Ki67+cells, LSCs, Ki67+LSCs, and AEC2 in LPS-challenged vagotomized mice. Stem Cell Res Ther. 2020 Jun 10;11(1):230
Rats HIV-1 gp120-induced mechanical allodynia model Intrathecal injection 1 µM or 10 µM Single administration, observed for 4 hours To evaluate the reversal effect of GTS-21 on gp120-induced mechanical allodynia. Results showed that GTS-21 (1 μM) significantly reversed mechanical allodynia from 1-3 hours after administration, while the 10 μM dose reversed allodynia from 2-4 hours after administration. Brain Behav Immun. 2010 Aug;24(6):959-67

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00783068 Endotoxemia S... More >>epsis Vagal Activity Less << Not Applicable Completed - Netherlands ... More >> Radboud University Nijmegen Medical Centre Nijmegen, GLD, Netherlands, 6525 GA Less <<
NCT00414622 Alzheimer Disease PHASE2 COMPLETED 2025-04-07 Clinical Dept., 280 South San ... More >>Francisco, California, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.62mL

0.52mL

0.26mL

13.11mL

2.62mL

1.31mL

26.23mL

5.25mL

2.62mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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