1. Membrane Transporter/Ion Channel
  2. EAAT
  3. Dihydrokainic acid

Dihydrokainic acid 是一种谷氨酸转运体 (尤其是 GLT1) 抑制剂。Dihydrokainic acid 对 GLT1 具有较高亲和力,能有效抑制其转运功能。Dihydrokainic acid 通过抑制谷氨酸的摄取,致使细胞外谷氨酸浓度升高,进而影响神经元的兴奋性和神经信号传递。Dihydrokainic acid 主要应用于神经科学领域中谷氨酸相关神经功能、癫痫以及学习记忆等方面的研究。

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Dihydrokainic acid

Dihydrokainic acid Chemical Structure

CAS No. : 52497-36-6

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Other Forms of Dihydrokainic acid:

MCE 顾客使用本产品发表的 1 篇科研文献

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Dihydrokainic acid is a glutamate transporters (especially GLT1) inhibitor. Dihydrokainic acid targets GLT1 with high affinity, effectively inhibiting its transport function. Dihydrokainic acid exerts its effect by inhibiting the uptake of glutamate, leading to an increase in extracellular glutamate concentration, thereby affecting neuronal excitability and neurotransmission. Dihydrokainic acid is mainly applied in the field of neuroscience for research on glutamate-related neural functions, epilepsy, learning, and memory[1][2][3][4][5].

IC50 & Target

EAAT2

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
> 3000 μM
Compound: DHK, dihydrokainic acid
Inhibition of glutamate-induced depolarization in human EAAT1 expressed in HEK293 cells by FMP assay
Inhibition of glutamate-induced depolarization in human EAAT1 expressed in HEK293 cells by FMP assay
[PMID: 18578477]
HEK293 IC50
> 3000 μM
Compound: DHK, dihydrokainic acid
Inhibition of glutamate-induced depolarization in human EAAT3 expressed in HEK293 cells by FMP assay
Inhibition of glutamate-induced depolarization in human EAAT3 expressed in HEK293 cells by FMP assay
[PMID: 18578477]
HEK293 IC50
89 μM
Compound: DHK, dihydrokainic acid
Inhibition of glutamate-induced depolarization in human EAAT2 expressed in HEK293 cells by FMP assay
Inhibition of glutamate-induced depolarization in human EAAT2 expressed in HEK293 cells by FMP assay
[PMID: 18578477]
体外研究
(In Vitro)

Dihydrokainic acid (5 mM;处理小脑切片 15 min) 浓度依赖性地抑制小脑切片对 D-[3H] 天冬氨酸的摄取[2]

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

体内研究
(In Vivo)

Dihydrokainic acid (1-10 mM;通过透析探针灌注;持续 60 min;单次给药) 在大鼠齿状回模型中,能诱发癫痫样活动,导致细胞外牛磺酸、丙氨酸、磷酸乙醇胺以及谷氨酸和天冬氨酸浓度增加,同时使群体峰电位幅度增大、PS2:PSI 比值升高[3]。 Dihydrokainic acid (12.5-25 nmol;单侧脑室内注射;单次给药) 在小鼠新颖物体识别 (NOR) 记忆模型中,会损害短期 NOR 记忆表现、长期 NOR 记忆获取、巩固和检索能力[4]。 Dihydrokainic acid (1-5mM;通过透析电极灌注;15 min;单次给药) 在大鼠海马体 (齿状回或 CA1 区)模型中,可使细胞外谷氨酸和牛磺酸浓度显著增加,在齿状回中降低场兴奋性突触后电位但增大群体峰电位,在 CA1 区则使兴奋性突触后电位和峰电位幅度均降低[5]

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

Animal Model: Kunming strain male mice (male, 35-40 g, not specified age) + novel object recognition (NOR) memory model[4]
Dosage: 6.25, 12.5, 25 nmol (0.01 M PBS, pH 7.4)
Administration: Unilaterally injected into the cerebral ventricle, once at 0.5 h before sampling or 0.5 h before testing
Result: Impaired short-term and long-term NOR memory performance, affecting memory acquisition, consolidation, and retrieval.
分子量

215.25

Formula

C10H17NO4

CAS 号
性状

固体

颜色

White to off-white

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 : 5 mg/mL (23.23 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 4.6458 mL 23.2289 mL 46.4578 mL
5 mM 0.9292 mL 4.6458 mL 9.2916 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
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: ≥99.0%

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 4.6458 mL 23.2289 mL 46.4578 mL 116.1446 mL
5 mM 0.9292 mL 4.6458 mL 9.2916 mL 23.2289 mL
10 mM 0.4646 mL 2.3229 mL 4.6458 mL 11.6145 mL
15 mM 0.3097 mL 1.5486 mL 3.0972 mL 7.7430 mL
20 mM 0.2323 mL 1.1614 mL 2.3229 mL 5.8072 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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产品名称:
Dihydrokainic acid
目录号:
HY-100784
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