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

Name: GTS-21 dihydrochloride
Brand: MedChemExpress
SKU: HY-14564A
Rating: 5.0 (14 reviews)

Cat. No.: HY-14564A Purity: 99.65%: Data Sheet
COA

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Handling Instructions
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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 (K_i=20 nM for humanα4β2) and 5-HT3A receptor (IC₅₀=3.1 μM) antagonist.

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

CAS No. : 156223-05-1

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 14 publication(s) in Google Scholar

Other Forms of GTS-21 dihydrochloride:

GTS-21 Get quote

14 Publications Citing Use of MCE GTS-21 dihydrochloride

Flow Cytometry

Cell Imaging/Staining

: GTS-21 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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).

: GTS-21 dihydrochloride purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2022 May:149:112733.; GTS-21 dihydrochloride (10 μM). The relative expression levels of ZO-1, Occludin, and Claudin-1 in Caco2 cells were analyzed by Western blot.

: GTS-21 dihydrochloride 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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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]^[2]

5-HT_3A Receptor

α7-nAChR

human α4β2

20 nM (Ki)

5-HT_3A Receptor

3.1 μM (IC₅₀)

In Vitro

GTS-21 bound to human α4β2 nAChR (K_i=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.

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.

Molecular Weight

381.30

Formula

C₁₉H₂₂Cl₂N₂O₂

CAS No.

156223-05-1

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
10 mM	0.2623 mL	1.3113 mL	2.6226 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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)

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: 99.65%

Select Batch:

Data Sheet (280 KB) SDS (254 KB)

COA (255 KB) LCMS (118 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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.

GTS-21 dihydrochloride Related Classifications

Inflammation/Immunology

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.

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

Customer Review

Other Forms of GTS-21 dihydrochloride:

GTS-21 dihydrochloride Related Antibodies

14 Publications Citing Use of MCE GTS-21 dihydrochloride

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All 5-HT Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

GTS-21 dihydrochloride Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

GTS-21 dihydrochloride Related Classifications

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