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官网链接https://www.medchemexpress.cn/guanidinoethyl-sulfonate.html
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。
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.
Guanidinoethyl sulfonate 相关抗体:
BNSP Antibody
FACL4 Antibody (YA851)
BrdU Antibody (YA578)
GAPDH Antibody (YA418)
Glucose 6 Phosphate Dehydrogenase Antibody (YA411)
METTL3 Antibody (YA294)
TSG101 Antibody (YA025)
Alkaline Phosphatase Antibody (YA629)
Calnexin Antibody (YA573)
Lamin A/C Antibody (YA314)
Lamin B1 Antibody (YA313)
LAMP1 Antibody (YA311)
LAMP2 Antibody (YA713)
LAMP2a Antibody (YA309)
NQO1 Antibody (YA697)
NQO1 Antibody (YA261)
OPA1 Antibody (YA256)
RBM3 Antibody (YA101)
Synaptophysin Antibody (YA043)
Laminin beta 1 Antibody (YA312)
Heme Oxygenase 1 Antibody (YA389)
Ki67 Antibody (YA717)
Ki67 Antibody (YA322)
Asparagine Synthetase Antibody (YA608)
ASS1 Antibody (YA607)
Calnexin Antibody
Ki67 Antibody (YA001)
Osteopontin Antibody
Synaptophysin Antibody (YA664)
TREM2 Antibody
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
543-18-0
性状
固体
颜色
White to off-white
结构分类
Others
初始来源
内源性代谢物疾病标志物其他疾病
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
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。
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.
Guanidinoethyl sulfonate 相关抗体:
BNSP Antibody
FACL4 Antibody (YA851)
BrdU Antibody (YA578)
GAPDH Antibody (YA418)
Glucose 6 Phosphate Dehydrogenase Antibody (YA411)
METTL3 Antibody (YA294)
TSG101 Antibody (YA025)
Alkaline Phosphatase Antibody (YA629)
Calnexin Antibody (YA573)
Lamin A/C Antibody (YA314)
Lamin B1 Antibody (YA313)
LAMP1 Antibody (YA311)
LAMP2 Antibody (YA713)
LAMP2a Antibody (YA309)
NQO1 Antibody (YA697)
NQO1 Antibody (YA261)
OPA1 Antibody (YA256)
RBM3 Antibody (YA101)
Synaptophysin Antibody (YA043)
Laminin beta 1 Antibody (YA312)
Heme Oxygenase 1 Antibody (YA389)
Ki67 Antibody (YA717)
Ki67 Antibody (YA322)
Asparagine Synthetase Antibody (YA608)
ASS1 Antibody (YA607)
Calnexin Antibody
Ki67 Antibody (YA001)
Osteopontin Antibody
Synaptophysin Antibody (YA664)
TREM2 Antibody
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
543-18-0
性状
固体
颜色
White to off-white
结构分类
Others
初始来源
内源性代谢物疾病标志物其他疾病
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