Guanidinoethyl sulfonate (Synonyms: NSC 667063,Taurocyamine) |
| Catalog No.GC15461 |
Guanidinoethyl sulfonate (GES) is a taurine analogue that competitively inhibits taurine uptake, causes taurine depletion by acting as a competitive inhibitor of TauT, PAT1 and GAT2 as well as interfering with taurine biosynthesis.
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Cas No.: 543-18-0
Sample solution is provided at 25 µL, 10mM.
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Guanidinoethyl sulfonate (GES) is a taurine analogue that competitively inhibits taurine uptake, causes taurine depletion by acting as a competitive inhibitor of TauT, PAT1 and GAT2 as well as interfering with taurine biosynthesis[1][2]. Guanidinoethyl sulfonate is commonly used to study neurodegenerative diseases and epilepsy [1][3][4].
Guanidinoethyl sulfonate (50, 40, 30, 20, 10, 5, and 2.5mM; 1h) decreased the cellular uptake of VGB, GABA, and taurine in ARPE-19 cells[4]. Guanidinoethyl sulfonate (10, 100, 1000, 10,000 and 30,000μM; 120ms) activated inward currents in a dose-dependent fashion on cerebellar granule cells[5].
Guanidinoethyl sulfonate (1mg/kg/day, 10 days, i.v.) decreased the VGB retinal levels in rats by 1.5-folds (P< 0.001, n = 6) compared with rats administered with similar dose of VGB alone[4].
References:
[1] Sergeeva OA, Chepkova AN, Haas HL. Guanidinoethyl sulphonate is a glycine receptor antagonist in striatum. British journal of pharmacology. 2002 Nov;137(6):855-60.
[2] Richter M, Moroniak SJ, Michel H. Identification of competitive inhibitors of the human taurine transporter TauT in a human kidney cell line. Pharmacological Reports. 2019 Feb 1;71(1):121-9.
[3] Suárez LM, Muñoz MD, González JC, Bustamante J, Del Río RM, Solís JM. The taurine transporter substrate guanidinoethyl sulfonate mimics the action of taurine on long-term synaptic potentiation. Amino acids. 2016 Nov;48:2647-56.
[4] Police A, Shankar VK, Murthy SN. Role of taurine transporter in the retinal uptake of vigabatrin. AAPS PharmSciTech. 2020 Jul;21:1-9.
[5] Mellor JR, Gunthorpe MJ, Randall AD. The taurine uptake inhibitor guanidinoethyl sulphonate is an agonist at γ-aminobutyric acidA receptors in cultured murine cerebellar granule cells. Neuroscience letters. 2000 May 26;286(1):25-8.
| Cell experiment [1]: | |
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Cell lines |
Human adult retinal pigment epithelial (ARPE-19) cells |
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Preparation Method |
ARPE-19 cells were preincubated with uptake buffer containing different concentrations (50, 40, 30, 20, 10, 5, and 2.5mM) of TauT inhibitor Guanidinoethyl sulfonate (GES) for 30min. To the preincubated cells, VGB (50mM), GABA (20mM), and taurine (0.2mM) were added and cells were incubated for 30min at 37°C. At the end of 30-min incubation period, cellular uptake was determined. |
|
Reaction Conditions |
50, 40, 30, 20, 10, 5, and 2.5mM; 1h |
|
Applications |
Guanidinoethyl sulfonate decreased the cellular uptake of VGB, GABA, and taurine. |
| Animal experiment [1]: | |
|
Animal models |
Sprague Dawley (SD) rats treated with anti-epileptic drug (Vigabatrin, VGB) |
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Preparation Method |
Twenty-four male SD rats of age 7-8 weeks were used for assessing the effect of chronic administration of Guanidinoethyl sulfonate (GES) and taurine on retinal levels of VGB. The animals were housed in a room, where temperature and humidity were controlled with 12-h light:12-h dark cycle. Animals were divided into four groups each containing 6 animals. The first group of animals were untreated, where they were dosed with normal saline to estimate the basal levels of taurine in the retina. The second group of animals was dosed with normal saline for 10 days intravenously and on 10th day the animals were dosed with 400mg/kg of VGB by intraperitoneal route. The third group of animals were dosed with GES at 1mg/kg intravenously for 10 days and on 10th day the animals were dosed with 400mg/kg of VGB by intraperitoneal route. The fourth group of animals were dosed with taurine at 100mg/kg orally for 10 days and on 10th day the animals were dosed with 400mg/kg of VGB by intraperitoneal route. On 10th day, after 2h of dosing. the animals of all groups were euthanized, and the eyes are enucleated and snap frozen. The retina was isolated at 4°C and homogenized using phosphate buffered saline and stored at -70 ± 5°C until bioanalysis. |
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Dosage form |
1mg/kg/day, 10 days, i.v. |
|
Applications |
Guanidinoethyl sulfonate decreased the VGB retinal levels in rats by 1.5-folds (P< 0.001, n = 6) compared with rats administered with similar dose of VGB alone. |
|
References: |
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| Cas No. | 543-18-0 | SDF | |
| Synonyms | NSC 667063,Taurocyamine | ||
| Chemical Name | 2-[(aminoiminomethyl)amino]-ethanesulfonic acid | ||
| Canonical SMILES | OS(CCNC(N)=N)(=O)=O | ||
| Formula | C3H9N3O3S | M.Wt | 167.2 |
| Solubility | Water:40mg/ml | Storage | Store at -20°C,protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 5.9809 mL | 29.9043 mL | 59.8086 mL |
| 5 mM | 1.1962 mL | 5.9809 mL | 11.9617 mL |
| 10 mM | 0.5981 mL | 2.9904 mL | 5.9809 mL |
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Quality Control & SDS
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- Purity: >97.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)
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