1. 诱导疾病模型产品 Membrane Transporter/Ion Channel
  2. 神经系统疾病模型 EAAT
  3. 癫痫模型
  4. Kainic acid

Kainic acid  (Synonyms: 红藻氨酸)

目录号: HY-N2309 纯度: 99.85%
COA 产品使用指南

Kainic acid 是一种有效的兴奋性毒性剂。Kainic acid 也是离子型谷氨酸受体亚型的激动剂。Kainic acid 诱发癫痫发作。

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Kainic acid Chemical Structure

Kainic acid Chemical Structure

CAS No. : 487-79-6

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10 mM * 1 mL in Water ¥1642
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1 mg ¥700
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Other Forms of Kainic acid:

查看 EAAT 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Kainic acid is a potent excitotoxic agent. Kainic acid hydrate also is an agonist for a subtype of ionotropic glutamate receptor. Kainic acid induces seizures[1][2].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 EC50
0.7 μM
Compound: Kainate
Compound was tested for agonistic activity at Glutamate receptor 6 using HEK293 cells
Compound was tested for agonistic activity at Glutamate receptor 6 using HEK293 cells
[PMID: 10969973]
HEK293 EC50
1.8 μM
Compound: 1, KA
Agonist activity at rat recombinant GluR6(Q) RNA-edited isoform expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assay
Agonist activity at rat recombinant GluR6(Q) RNA-edited isoform expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assay
[PMID: 19588945]
HEK293 EC50
16.2 μM
Compound: Kainate
Compound was tested for agonistic activity at Glutamate receptor 5 using HEK293 cells
Compound was tested for agonistic activity at Glutamate receptor 5 using HEK293 cells
[PMID: 10969973]
HEK293 EC50
23 μM
Compound: Kainate
Agonist activity at rat recombinant GluA1 receptor flip isoform expressed in HEK293 cells assessed as effect on cyclothiazide-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
Agonist activity at rat recombinant GluA1 receptor flip isoform expressed in HEK293 cells assessed as effect on cyclothiazide-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
[PMID: 20096591]
HEK293 EC50
23 μM
Compound: 1, KA
Agonist activity at rat recombinant GluR1 flip isoform expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assay
Agonist activity at rat recombinant GluR1 flip isoform expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assay
[PMID: 19588945]
HEK293 EC50
37 μM
Compound: 1, KA
Agonist activity at rat recombinant GluR5(Q) RNA-edited isoform expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assay
Agonist activity at rat recombinant GluR5(Q) RNA-edited isoform expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assay
[PMID: 19588945]
HEK293 EC50
380 μM
Compound: Kainate
Agonist activity at rat recombinant GluA2 receptor flip isoform expressed in HEK293 cells assessed as effect on cyclothiazide-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
Agonist activity at rat recombinant GluA2 receptor flip isoform expressed in HEK293 cells assessed as effect on cyclothiazide-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
[PMID: 20096591]
HEK293 EC50
380 μM
Compound: 1, KA
Agonist activity at rat recombinant GluR2(Q) RNA-edited isoform expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assay
Agonist activity at rat recombinant GluR2(Q) RNA-edited isoform expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assay
[PMID: 19588945]
HEK293 EC50
40 μM
Compound: Kainate
Agonist activity at rat recombinant GluA3 receptor flip isoform expressed in HEK293 cells assessed as effect on cyclothiazide-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
Agonist activity at rat recombinant GluA3 receptor flip isoform expressed in HEK293 cells assessed as effect on cyclothiazide-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
[PMID: 20096591]
HEK293 EC50
40 μM
Compound: 1, KA
Agonist activity at rat recombinant GluR3 flip isomer expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assay
Agonist activity at rat recombinant GluR3 flip isomer expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assay
[PMID: 19588945]
HEK293 EC50
47 μM
Compound: Kainate
Agonist activity at rat recombinant GluA4 receptor flip isoform expressed in HEK293 cells assessed as effect on cyclothiazide-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
Agonist activity at rat recombinant GluA4 receptor flip isoform expressed in HEK293 cells assessed as effect on cyclothiazide-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
[PMID: 20096591]
HEK293 EC50
47 μM
Compound: 1, KA
Agonist activity at rat recombinant GluR4 flip isomer expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assay
Agonist activity at rat recombinant GluR4 flip isomer expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4/AM assay
[PMID: 19588945]
Neuron EC50
17.3 μM
Compound: kainate
Excitotoxicity against C57BL/6N mouse hippocampal neurons after 48 hrs by MTT assay
Excitotoxicity against C57BL/6N mouse hippocampal neurons after 48 hrs by MTT assay
[PMID: 18083036]
体内研究
(In Vivo)

Kainic acid 诱导的癫痫模型是研究颞叶癫痫的有效工具,可通过全身、海马或杏仁体给药,在多种动物模型中重现。系统性给药的 Kainic acid 模型与人类颞叶癫痫 (TLE) 表现相似。当 Kainic acid (5 nM) 被注射到新纹状体、黑质或小脑时,0.5 小时后超过一半的化合物已从注射点及大脑中消失,同时在其他脑区检测到的放射性物质浓度低于 7 pM/mg 组织[3][4][6]

1. 诱导小鼠癫痫模型[5]
致病原理
Kainic acid 是 L-谷氨酸的类似物和离子型 KA 受体激动剂,可损伤海马锥体神经元。
具体造模方法:
小鼠:C57BL/6J • 雄性 • 7 周龄 • 22 g
给药方式:10 μg, 5 μL • i.c.v.
Note
(1) 用立体定向仪定位右侧脑室。
(2) 手术结束后,缝合皮肤,将小鼠置于温暖处直至苏醒。
(3) 侧脑室注射后 48 小时,用异氟烷麻醉小鼠,然后依次向心内灌注生理盐水和PFA (4%,30mL)。 快速取出小鼠大脑,通过石蜡包埋或冰冻切片处理。”
造模成功指标
脑电图 (EEG) 记录:与对照组相比,局部最大幅度更高,尖峰频率更低。
组织学分析:显示海马神经元中三角固缩核和细胞质收缩,并诱导神经元丢失。
相关产品: /
拮抗产品Sitagliptin (HY-13749)

2. 诱导大鼠癫痫模型[6]
致病原理
Kainic acid 可以与海马角、杏仁核和梨状皮层神经元中丰富的 NMDA 受体结合,并导致这些区域的不同程度的神经元死亡。
具体造模方法:
大鼠:Sprague-Dawley 大鼠 • 雄性
给药方式:10 mg/kg • 腹腔注射 • a 单剂量
Note
(1) 注射后约 45 分钟发生癫痫发作,通常持续 2-3 小时。
(2) Kainic acid 处理的动物在急性中毒期间可能会死亡,建议增加每组的动物数量。
(3) 72 小时后,麻醉大鼠,立即经心灌注50 mL 0.9% 盐水,随后灌注 500 mL 0.1M 中性磷酸盐缓冲甲醛 (4%)。取出大脑并在相同的固定剂中于 4°C 后固定过夜并脱水,包埋在石蜡中,并在背侧海马水平切成连续的 6 μm 厚的冠状切片。
造模成功指标
行为变化:首先表现出不动和僵硬的姿势,然后是重复点头、‘湿狗式摇晃’,然后直立和跌倒。最终,老鼠出现全身强直阵挛性癫痫发作,伴有持续抽搐, 持续几个小时。
组织学分析:导致海马 CA1 和 CA3 区锥体神经元丢失。
GFAP 免疫反应细胞的大小、树枝化和可染色性增加。
相关产品: /
拮抗产品Melatonin (HY-B0075)

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

Animal Model: 8 weeks, 200-250 g male adult Wistar rats[1]
Dosage: 5 mg/kg
Administration: I.p.; hourly at least 3 h until status epilepticus
Result: Induced seizures in rats.
分子量

213.23

Formula

C10H15NO4

CAS 号
性状

固体

颜色

White to off-white

中文名称

红藻氨酸;卡英酸

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: 

DMSO 中的溶解度 : 40 mg/mL (187.59 mM; ultrasonic and adjust pH to 3 with 1 M HCL; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : 10 mg/mL (46.90 mM; 超声助溶 (<60°C))

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.6897 mL 23.4485 mL 46.8971 mL
5 mM 0.9379 mL 4.6897 mL 9.3794 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:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
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: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5 mg/mL (23.45 mM); 澄清溶液

    此方案可获得 ≥ 5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (23.45 mM); 澄清溶液

    此方案可获得 ≥ 5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
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
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.96%

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 / DMSO 1 mM 4.6897 mL 23.4485 mL 46.8971 mL 117.2426 mL
5 mM 0.9379 mL 4.6897 mL 9.3794 mL 23.4485 mL
10 mM 0.4690 mL 2.3449 mL 4.6897 mL 11.7243 mL
15 mM 0.3126 mL 1.5632 mL 3.1265 mL 7.8162 mL
20 mM 0.2345 mL 1.1724 mL 2.3449 mL 5.8621 mL
25 mM 0.1876 mL 0.9379 mL 1.8759 mL 4.6897 mL
30 mM 0.1563 mL 0.7816 mL 1.5632 mL 3.9081 mL
40 mM 0.1172 mL 0.5862 mL 1.1724 mL 2.9311 mL
DMSO 50 mM 0.0938 mL 0.4690 mL 0.9379 mL 2.3449 mL
60 mM 0.0782 mL 0.3908 mL 0.7816 mL 1.9540 mL
80 mM 0.0586 mL 0.2931 mL 0.5862 mL 1.4655 mL
100 mM 0.0469 mL 0.2345 mL 0.4690 mL 1.1724 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。

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产品名称:
Kainic acid
目录号:
HY-N2309
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