2. Metabolic Enzyme/Protease
  3. Endogenous Metabolite
  4. Guanidinoethyl sulfonate

Guanidinoethyl sulfonate  (Synonyms: Taurocyamine)

Cat. No.: HY-113329 Purity: ≥98.0%
SDS
COA
Handling Instructions Technical Support

Guanidinoethyl sulfonate is an orally available, blood-brain permeable competitive inhibitor of taurine transporters and a competitive antagonist of glycine receptors (GlyR) (IC50=565 μM). Guanidinoethyl sulfonate has both weak agonist and antagonist effects on GABAA receptors. Guanidinoethyl sulfonate inhibits taurine transmembrane transport and competitively binds to the GlyR ligand binding domain, thereby blocking glycine-mediated chloride influx, and may regulate brain pH to exert neuroprotective effects. Guanidinoethyl sulfonate can be used for neuroprotection studies of ischemic brain injury.

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

Guanidinoethyl sulfonate Chemical Structure

Guanidinoethyl sulfonate Chemical Structure

CAS No. : 543-18-0

Size Price Stock Quantity
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Guanidinoethyl sulfonate Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Guanidinoethyl sulfonate is an orally available, blood-brain permeable competitive inhibitor of taurine transporters and a competitive antagonist of glycine receptors (GlyR) (IC50=565 μM). Guanidinoethyl sulfonate has both weak agonist and antagonist effects on GABAA receptors. Guanidinoethyl sulfonate inhibits taurine transmembrane transport and competitively binds to the GlyR ligand binding domain, thereby blocking glycine-mediated chloride influx, and may regulate brain pH to exert neuroprotective effects. Guanidinoethyl sulfonate can be used for neuroprotection studies of ischemic brain injury[1][2][3].

IC50 & Target

Human Endogenous Metabolite

 

In Vitro

Electrophysiological experiments (Glycine receptor activity): Guanidinoethyl sulfonate (0.5 mM; transient) competitively antagonized glycine-induced currents in mouse striatal neurons, shifting the glycine dose-response curve to the right, with the EC50 increasing from 62 μM (control group) to 154 μM (treated group)[1].
Electrophysiological experiments (GABA receptor activity): Guanidinoethyl sulfonate (1 mM; transient) exhibited both weak agonist (evoked currents of 5.6%-9.9% of the maximal GABA response) and antagonist (inhibiting the 10 μM GABA response to 26.3%) effects on GABAA receptors in mouse striatal neurons[1].

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

Guanidinoethyl sulfonate Related Antibodies

Cell Viability Assay[1]

Cell Line: Mouse striatal giant aspiny neurons (GAN) and medium spiny neurons (MSN)
Concentration: 0.5 mM, 1 mM
Incubation Time:
Result: At 0.5 mM, shifted the glycine dose-response curve rightward without affecting maximal response, increasing EC50 from 62 μM to 154 μM and decreasing the Hill coefficient from 2.5 to 1.3.
At 1 mM, reduced glycine (100 μM)-evoked currents to 36 ± 2.7% in GAN and 35 ± 3.9% in MSN, with voltage-independent block confirmed by unchanged reversal potentials near chloride equilibrium potential. GABA 受体交互实验（GABAAR interaction assay）Cell Line: Mouse striatal medium spiny neurons and cholinergic interneurons[1] Concentration: 1 mM, 10 mM Incubation Time: seconds for current recording Result: At 10 mM, evoked small currents (9.9% of maximal GABA response in medium spiny neurons, 5.6% in cholinergic interneurons), with a dose-dependent response EC50=534 μM).
At 1 mM, co-application with 10 μM GABA reduced GABA-evoked currents to 26.3% of control, and these effects were partially blocked by the GABAA antagonist gabazine, indicating mixed agonistic and antagonistic interactions with GABAA receptors.
In Vivo

Forebrain ischemia model:
Guanidinoethyl sulfonate (625 mg/kg; intraperitoneal injection; once a day; 2 weeks) pretreatment in adult male gerbils significantly increases the survival rate of hippocampal CA1 neurons after ischemia and alleviates delayed neuronal death[2].
Pregnancy model:
Guanidinoethyl sulfonate (1% drinking water; free drinking; gestational day 11-21) causes a significant decrease in taurine concentrations in the fetus' body, liver, brain and placenta (32%-87%), reduces fetal body weight and organ weights, and increases maternal urinary taurine excretion in the Wistar pregnant rat model[3].

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

Animal Model: Adult male gerbils (70 g), forebrain ischemia-reperfusion model[2]
Dosage: 625 mg/kg, dissolved in distilled water (neutralized to pH 7.0 with NaOH)
Administration: Intraperitoneal injection, daily for 2 weeks, followed by 5-minute bilateral carotid artery occlusion and 7-day reperfusion
Result: Significantly increased the number of surviving CA1 neurons (61.1 cells/mm) compared to saline-treated ischemic controls (17.75 cells/mm).
Decreased brain taurine levels, while increased intracellular pH, indicating a protective effect against ischemic neuronal death without affecting baseline neuronal density in non-ischemic controls.
Animal Model: Pregnant Wistar rats (initial weight 190-230 g), gestational taurine depletion model[3]
Dosage: 1% guanidinoethyl sulfonate (GES) in drinking water
Administration: Free access to GES-containing water from gestational day 11 to 21 (10 days total)
Result: Led to significant taurine depletion in fetal tissues (54% in whole body, 37% in liver, 87% in brain, 32% in placenta) and maternal tissues (33% in liver, 32% in brain, 46% in plasma).
Fetal wet weights of whole body, liver, brain, and placenta were reduced by 17%, 24%, 5%, and 13%, respectively, compared to controls.
Maternal urinary taurine excretion increased significantly throughout the treatment period, with no changes in maternal organ weights or food/water intake.
Molecular Weight

167.19

Formula

C3H9N3O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N=C(NCCS(=O)(O)=O)N
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 41.67 mg/mL (249.24 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.9812 mL 29.9061 mL 59.8122 mL
5 mM 1.1962 mL 5.9812 mL 11.9624 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. 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)

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:

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: 25 mg/mL (149.53 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: ≥98.0%

SDS (252 KB)

COA (245 KB) HNMR (232 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. 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
H2O 1 mM 5.9812 mL 29.9061 mL 59.8122 mL 149.5305 mL
5 mM 1.1962 mL 5.9812 mL 11.9624 mL 29.9061 mL
10 mM 0.5981 mL 2.9906 mL 5.9812 mL 14.9530 mL
15 mM 0.3987 mL 1.9937 mL 3.9875 mL 9.9687 mL
20 mM 0.2991 mL 1.4953 mL 2.9906 mL 7.4765 mL
25 mM 0.2392 mL 1.1962 mL 2.3925 mL 5.9812 mL
30 mM 0.1994 mL 0.9969 mL 1.9937 mL 4.9843 mL
40 mM 0.1495 mL 0.7477 mL 1.4953 mL 3.7383 mL
50 mM 0.1196 mL 0.5981 mL 1.1962 mL 2.9906 mL
60 mM 0.0997 mL 0.4984 mL 0.9969 mL 2.4922 mL
80 mM 0.0748 mL 0.3738 mL 0.7477 mL 1.8691 mL
100 mM 0.0598 mL 0.2991 mL 0.5981 mL 1.4953 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.

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Guanidinoethyl sulfonate 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:

Guanidinoethyl sulfonate543-18-0TaurocyamineEndogenous Metabolitetaurine transport antagonistInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Guanidinoethyl sulfonate
Cat. No.:
HY-113329
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (252 KB) Français - FR (252 KB) Deutsch - DE (252 KB) Norwegian - NO (252 KB) Español - ES (252 KB) Swedish - SV (252 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.