Guanidinoethyl sulfonate
(Synonyms: 脒基牛磺酸,NSC 667063,Taurocyamine) 目录号 : GC15461
Guanidinoethyl sulfonate（GES）是一种牛磺酸类似物，可竞争性抑制牛磺酸的摄取，通过作为TauT、PAT1和GAT2的竞争性抑制剂导致牛磺酸耗竭，并干扰牛磺酸的生物合成。
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.
Guanidinoethyl sulfonate（GES）是一种牛磺酸类似物，可竞争性抑制牛磺酸的摄取，通过作为TauT、PAT1和GAT2的竞争性抑制剂导致牛磺酸耗竭，并干扰牛磺酸的生物合成[1][2]。Guanidinoethyl sulfonate常用来研究神经退行性疾病和癫痫[1][3][4]。
Guanidinoethyl sulfonate（50、40、30、20、10、5和2.5mM；1h）降低了ARPE-19细胞对VGB、GABA和牛磺酸的细胞摄取[4]。Guanidinoethyl sulfonate（10、100、1000、10,000和30,000μM；120ms）以剂量依赖性方式激活小脑颗粒细胞的内向电流[5]。
与单独使用相似剂量VGB的大鼠相比，Guanidinoethyl sulfonate（1mg/kg/天，10天，静脉注射）使大鼠的VGB视网膜水平降低了1.5倍（P< 0.001，n = 6）[4]。
| 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) |
|
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. |
|
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 | |
| 别名 | 脒基牛磺酸,NSC 667063,Taurocyamine | ||
| 化学名 | 2-[(aminoiminomethyl)amino]-ethanesulfonic acid | ||
| Canonical SMILES | OS(CCNC(N)=N)(=O)=O | ||
| 分子式 | C3H9N3O3S | 分子量 | 167.2 |
| 溶解度 | ≤1mg/ml in PBS | 储存条件 | Store at -20°C,protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >97.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet