| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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Purity: ≥98%
GTS-21, formerly known as DMBX-A, is a analogue of the natural product anabaseine that acts as a partial agonist at neural nicotinic acetylcholine receptors. It binds to both the α4β2 and α7 subtypes, but activates only the α7 to any significant extent. Both GTS-21 itself and its demethylated active metabolite 4-OH-GTS-21 display nootropic and neuroprotective effects, and GTS-21 is being investigated for the treatment of Alzheimer's disease, nicotine dependence, and, most significantly, for schizophrenia.
| ln Vitro |
In addition to binding to human α4β2 and a7 nAChR 18 times and 18 times lower than (-)-nicotine, respectively, GTS-21 also binds to human α4β2 nAChR (Ki=20 nM) 100 times stronger than it does to human α7-nAChR. Twice. 1].
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|---|---|
| ln Vivo |
The histological indicators of radiation-induced lung injury are lessened by GTS 21 (4 mg/kg; intraperitoneally; days 1, 3, 7, 14, and 21) [3].
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| Animal Protocol |
Animal/Disease Models: C57BL6 mice were irradiated with 12 Gy to induce radiation-induced lung injury (RILI) mouse model [3]
Doses: 4 mg/kg Route of Administration: intraperitoneal (ip) injection; results on days 1, 3, 7, 14 and 21 Experimental Results: Reduce pulmonary inflammatory infiltration and fibrosis in radiation-treated mice. |
| References |
| Molecular Formula |
C19H22CL2N2O2
|
|---|---|
| Molecular Weight |
381.3
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| Exact Mass |
308.15248
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| Elemental Analysis |
C, 59.85; H, 5.82; Cl, 18.59; N, 7.35; O, 8.39
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| CAS # |
156223-05-1
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| Related CAS # |
148372-04-7;156223-05-1 (HCl);
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| PubChem CID |
6438361
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
485.6±45.0 °C at 760 mmHg
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| Melting Point |
216-217℃ (decomposition)
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| Flash Point |
247.5±28.7 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.580
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| LogP |
2.64
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
|
| Heavy Atom Count |
25
|
| Complexity |
447
|
| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC(OC)=CC=C1/C=C2CCCN=C\2C3=CC=CN=C3.Cl[H].Cl[H]
|
| InChi Key |
3-[(3E)-3-[(2,4-dimethoxyphenyl)methylidene]-5,6-dihydro-4H-pyridin-2-yl]pyridine dihydrochloride
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| InChi Code |
BXKYFUGAAFLYJL-BXGYHSFXSA-N
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| Chemical Name |
GTS-21 HCl GTS-21 hydrochloride GTS-21 GTS 21 GTS21 DMBX-A
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| Synonyms |
GTS-21 HCl GTS-21 hydrochloride GTS-21 GTS 21 GTS21 DMBX-A
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~50 mg/mL (~131.13 mM)
DMSO : ~16.5 mg/mL (~43.27 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.56 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.56 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 75 mg/mL (196.70 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6226 mL | 13.1130 mL | 26.2261 mL | |
| 5 mM | 0.5245 mL | 2.6226 mL | 5.2452 mL | |
| 10 mM | 0.2623 mL | 1.3113 mL | 2.6226 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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