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

Guanidinoethyl sulfonate  (Synonyms: Taurocyamine)

目录号: HY-113329 纯度: 99.91%
COA 产品使用指南 技术支持

Guanidinoethyl sulfonate (Taurocyamine) 是一种口服有效、可透过血脑屏障的牛磺酸转运体的竞争性抑制剂和甘氨酸受体 (GlyR) 的竞争性拮抗剂 (IC50=565 μM)。Guanidinoethyl sulfonate 对 GABAA 受体兼具弱激动与拮抗作用。Guanidinoethyl sulfonate 抑制牛磺酸跨膜转运、竞争性结合 GlyR 配体结合域,从而阻断甘氨酸介导的氯离子内流,可能调节脑内 pH 值发挥神经保护效应。Guanidinoethyl sulfonate 可用于缺血性脑损伤的神经保护研究。

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Guanidinoethyl sulfonate

Guanidinoethyl sulfonate Chemical Structure

CAS No. : 543-18-0

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Other Forms of Guanidinoethyl sulfonate:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Guanidinoethyl sulfonate (Taurocyamine) 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

 

体外研究
(In Vitro)

电生理实验 (甘氨酸受体活性):
Guanidinoethyl sulfonate (0.5 mM;瞬时) 在小鼠纹状体神经元中竞争性拮抗甘氨酸诱导的电流,使甘氨酸剂量-反应曲线右移,EC50 从 62 μM (对照组) 升至 154 μM (处理组)[1]
电生理实验 (GABA 受体活性):
Guanidinoethyl sulfonate (1 mM;瞬时) 对小鼠纹状体神经元的 GABAA 受体兼具弱激动作用和拮抗作用[1]

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

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.
体内研究
(In Vivo)

前脑缺血模型:Guanidinoethyl sulfonate (625 mg/kg;腹腔注射;每日 1 次;2 周) 在成年雄性沙鼠中,预处理可显著提高缺血后海马 CA1 神经元存活率,减轻延迟性神经元死亡[2]
妊娠模型:Guanidinoethyl sulfonate (1% 饮用水;自由饮用;妊娠第 11-21 天) 在 Wistar 孕鼠模型中导致胎儿全身、肝脏、脑及胎盘的牛磺酸浓度显著下降 (32%-87%),胎儿体重及器官重量降低,母体尿牛磺酸排泄增加[3]

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.
分子量

167.19

Formula

C3H9N3O3S

CAS 号
性状

固体

颜色

White to off-white

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

H2O 中的溶解度 : 41.67 mg/mL (249.24 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 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, 6 months; -20°C, 1 month。-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。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

  • 方案 一

    请依序添加每种溶剂: PBS

    Solubility: 25 mg/mL (149.53 mM); 澄清溶液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 99.91%

参考文献

完整储备液配制表

* 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, 6 months; -20°C, 1 month。-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。

可选溶剂 浓度 溶剂体积 质量 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

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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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