2. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein
  3. nAChR 5-HT Receptor
  4. GTS-21 dihydrochloride

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

Cat. No.: HY-14564A Purity: 99.92%
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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.

For research use only. We do not sell to patients.

GTS-21 dihydrochloride Chemical Structure

GTS-21 dihydrochloride Chemical Structure

CAS No. : 156223-05-1

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10 mM * 1 mL in DMSO
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Based on 10 publication(s) in Google Scholar

Other Forms of GTS-21 dihydrochloride:

GTS-21 dihydrochloride Related Antibodies

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Description

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[1][2].

IC50 & Target[1][2]

α7-nAChR

 

human α4β2

20 nM (Ki)

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.

GTS-21 dihydrochloride Related Antibodies
In Vivo

GTS 21 (4 mg/kg; i.p.; 1, 3, 7, 14 and 21 days) reduces radiation induced histological signs of pulmonary injury[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL6 mice were irradiated with 12 Gy to induce a mouse model of Radiation induced lung injury (RILI)[3]
Dosage: 4 mg/kg
Administration: I.p.; 1, 3, 7, 14 and 21 days
Result: Reduces lung inflammatory infiltrate and fibrosis in radiation treated mice.
Clinical Trial
Molecular Weight

381.30

Formula

C19H22Cl2N2O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

COC1=CC(OC)=CC=C1/C=C2CCCN=C\2C3=CC=CN=C3.Cl[H].Cl[H]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (131.13 mM; Need ultrasonic)

DMSO : 16.5 mg/mL (43.27 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.56 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.56 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 75 mg/mL (196.70 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.92%

COA (255 KB) LCMS (266 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 2.6226 mL 13.1130 mL 26.2261 mL 65.5652 mL
5 mM 0.5245 mL 2.6226 mL 5.2452 mL 13.1130 mL
10 mM 0.2623 mL 1.3113 mL 2.6226 mL 6.5565 mL
15 mM 0.1748 mL 0.8742 mL 1.7484 mL 4.3710 mL
20 mM 0.1311 mL 0.6557 mL 1.3113 mL 3.2783 mL
25 mM 0.1049 mL 0.5245 mL 1.0490 mL 2.6226 mL
30 mM 0.0874 mL 0.4371 mL 0.8742 mL 2.1855 mL
40 mM 0.0656 mL 0.3278 mL 0.6557 mL 1.6391 mL
H2O 50 mM 0.0525 mL 0.2623 mL 0.5245 mL 1.3113 mL
60 mM 0.0437 mL 0.2186 mL 0.4371 mL 1.0928 mL
80 mM 0.0328 mL 0.1639 mL 0.3278 mL 0.8196 mL
100 mM 0.0262 mL 0.1311 mL 0.2623 mL 0.6557 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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GTS-21 dihydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GTS-21156223-05-1DMXB-A DMBX-anabaseineGTS21GTS 21nAChR5-HT ReceptorNicotinic acetylcholine receptorsSerotonin Receptor5-hydroxytryptamine Receptorpulmonaryinjuryfibrosislunganti?inflammatorycognitionInhibitorinhibitorinhibit

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