SML0326
GTS-21
≥97% (HPLC), α7 Nicotinic Acetylcholine Receptor Agonist, powder
Sinónimos:
3-(2,4-Dimethoxybenzylidene)-anabaseine dihydrochloride, DMBX-anabaseine, DMXB, DMXB-A, GTS21
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Fórmula empírica (notación de Hill):
C19H20N2O2 · 2HCl
Número CAS:
Peso molecular:
381.30
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
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Permítanos ayudarleNombre del producto
GTS-21, ≥97% (HPLC)
SMILES string
Cl.Cl.COc1ccc(\C=C2/CCCN=C2c3cccnc3)c(OC)c1
InChI
1S/C19H20N2O2.2ClH/c1-22-17-8-7-14(18(12-17)23-2)11-15-5-4-10-21-19(15)16-6-3-9-20-13-16;;/h3,6-9,11-13H,4-5,10H2,1-2H3;2*1H/b15-11+;;
InChI key
BXKYFUGAAFLYJL-BXGYHSFXSA-N
assay
≥97% (HPLC)
form
powder
color
faintly yellow to dark yellow
solubility
H2O: >5 mg/mL
storage temp.
2-8°C
Quality Level
Categorías relacionadas
Application
GTS-21 has been used:
- as an α7 nicotinic acetylcholine receptors (nAChR) partial agonist to elucidate its anti-inflammatory effects in mouse macrophages
- to test its protective effect on the renal injury induced by lipopolysaccharide (LPS)
- to test its effect on microvascular inflammation in endotoxemia induced by LPS
Biochem/physiol Actions
GTS-2, a derivative of anisine is an immunomodulatory drug. It is used for treating pancreatitis and septicemia. GTS-2 inhibits the pro-inflammatory cytokines especially the interleukin-6 (IL6) and tumor necrosis factor (TNF) in sepsis and endotoxemia.
GTS-21 is a selective agonist at α-7 nicotinic receptors with anti-inflammatory and cognition enhancing activities. GTS-21 has also been investigated for the treatment of schizophrenia.
GTS-21 is a selective agonist at α-7 nicotinic receptors.
Features and Benefits
This compound is featured on the Acetylcholine Receptors (Nicotinic) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
Clase de almacenamiento
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Ryan E Hibbs et al.
The EMBO journal, 28(19), 3040-3051 (2009-08-22)
The pentameric acetylcholine-binding protein (AChBP) is a soluble surrogate of the ligand binding domain of nicotinic acetylcholine receptors. Agonists bind within a nest of aromatic side chains contributed by loops C and F on opposing faces of each subunit interface.
Bianca Brawek et al.
International journal of molecular sciences, 22(3) (2021-01-28)
Microglia, the innate immune cells of the brain, are commonly perceived as resident macrophages of the central nervous system (CNS). This definition, however, requires further specification, as under healthy homeostatic conditions, neither morphological nor functional properties of microglia mirror those
Caijuan Shi et al.
Journal of molecular modeling, 19(2), 871-878 (2012-10-23)
Nicotinic acetylcholine receptors (nAChRs) are drug targets for neuronal disorders and diseases. Partial agonists for nAChRs are currently being developed as drugs for the treatment of neurological diseases for their relative safety originated from reduced excessive stimulation. In the current
Matthijs Kox et al.
Biochemical pharmacology, 78(7), 863-872 (2009-07-07)
The vagus nerve can limit inflammation via the alpha7 nicotinic acetylcholine receptor (alpha7nAChR). Selective pharmacological stimulation of the alpha7nAChR may have therapeutic potential for the treatment of inflammatory conditions. We determined the anti-inflammatory potential of GTS-21, an alpha7nAChR-selective partial agonist
Prodyot K Chatterjee et al.
PloS one, 7(5), e35361-e35361 (2012-05-16)
Sepsis is one of the leading causes of acute kidney injury (AKI). Septic patients who develop acute kidney injury (AKI) are at increased risk of death. To date there is no effective treatment for AKI or septic AKI. Based on
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