2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR GABA Receptor
  4. Cyclothiazide

Cyclothiazide  (Synonyms: 环噻嗪)

目录号: HY-101165 纯度: 98.29%
COA 产品使用指南 技术支持

Cyclothiazide 是离子型 AMPA 谷氨酸受体的正向变构调节剂。Cyclothiazide 可抑制 GABAA 受体。Cyclothiazide 常用于快速抑制 AMPA 受体脱敏，并显著降低 AMPA 电流的增强速度。Cyclothiazide 可增强海马神经元对海人酸 (kainate) 的反应。Cyclothiazide 对谷氨酸能神经传递有影响。Cyclothiazide 还会诱发伴随行为性癫痫发作的癫痫样脑电图活动。

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Cyclothiazide Chemical Structure

Cyclothiazide Chemical Structure

CAS No. : 2259-96-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥660
In-stock
1 mg ￥275
In-stock
5 mg ￥660
In-stock
10 mg ￥990
In-stock
25 mg ￥1980
In-stock
50 mg ￥3300
In-stock
100 mg   询价  
200 mg   询价  

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Customer Review

Other Forms of Cyclothiazide:

Cyclothiazide 相关抗体

Top Publications Citing Use of Products

查看 iGluR 亚型特异性产品:

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AMPA Receptor NMDA Receptor Kainate Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Cyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABAA receptors. Cyclothiazide is frequently used to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Cyclothiazide can potentiate responses to kainate in hippocampal neurons. Cyclothiazide has effects on glutamatergic neurotransmission. Cyclothiazide also induces epileptiform EEG activity accompanying behavioral seizures[1][2][3][4].

IC50 & Target

AMPA Receptor

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 EC50
> 100 μM
Compound: CTZ, Cyclothiazide
Activity at human recombinant GluA2 receptor flop isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
Activity at human recombinant GluA2 receptor flop isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
[PMID: 20096591]
HEK293 EC50
13.7 μM
Compound: CTZ, Cyclothiazide
Activity at human recombinant GluA3 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
Activity at human recombinant GluA3 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
[PMID: 20096591]
HEK293 EC50
19.8 μM
Compound: CTZ, Cyclothiazide
Activity at human recombinant GluA1 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
Activity at human recombinant GluA1 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
[PMID: 20096591]
HEK293 EC50
2.24 μM
Compound: CTZ, Cyclothiazide
Activity at human recombinant GluA2 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
Activity at human recombinant GluA2 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
[PMID: 20096591]
HEK293 EC50
3.91 μM
Compound: CTZ, Cyclothiazide
Activity at human recombinant GluA4 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
Activity at human recombinant GluA4 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
[PMID: 20096591]
HEK293 EC50
3800 nM
Compound: 2, cyclothiazide
Activity against human GLUR4 flip expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay
Activity against human GLUR4 flip expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay
[PMID: 16879964]
HEK293 EC50
7.6 μM
Compound: cyclothiazide
Agonist activity at human GluA2(Q)i expressed in HEK293 cells assessed as enhancement of glutamate-evoked desensitized current by whole cell patch clamp method
Agonist activity at human GluA2(Q)i expressed in HEK293 cells assessed as enhancement of glutamate-evoked desensitized current by whole cell patch clamp method
[PMID: 26653877]
Oocyte EC50
10 μM
Compound: CTZ, Cyclothiazide
Activity at recombinant GluA1 receptor flop isoform expressed in Xenopus oocytes co-expressing gamma2-TARP assessed as effect on 10 uM glutamate-induced current by voltage-clamp electrophysiological assay
Activity at recombinant GluA1 receptor flop isoform expressed in Xenopus oocytes co-expressing gamma2-TARP assessed as effect on 10 uM glutamate-induced current by voltage-clamp electrophysiological assay
[PMID: 20096591]
Oocyte EC50
2 μM
Compound: CTZ, Cyclothiazide
Activity at recombinant GluA1 receptor flip isoform expressed in Xenopus oocytes co-expressing gamma2-TARP assessed as effect on 10 uM glutamate-induced current by voltage-clamp electrophysiological assay
Activity at recombinant GluA1 receptor flip isoform expressed in Xenopus oocytes co-expressing gamma2-TARP assessed as effect on 10 uM glutamate-induced current by voltage-clamp electrophysiological assay
[PMID: 20096591]
Oocyte EC50
7.6 μM
Compound: Cyclothiazide
Agonist activity at rat flip iGluR2(Q) expressed in Xenopus laevis oocytes by whole cell patch-clamp method
Agonist activity at rat flip iGluR2(Q) expressed in Xenopus laevis oocytes by whole cell patch-clamp method
[PMID: 18811139]
体外研究
(In Vitro)

Clyclothiazide (Compound CTZ) (0-1000 μM，4 秒) 在 GluR1-HEK 细胞中剂量依赖性地显著增强 AMPA 电流，在浓度为 100 μM 时使峰值 AMPA 电流增加 90 倍 (EC50 = 28 μM)[1]。
Clyclothiazide (100 μM，0-150 秒) 可更快地抑制 GluR1-HEK 细胞中的脱敏[1]。
Clyclothiazide (30 μM) 可显著且可逆地增强啮齿动物神经元斑块对海人酸的反应[2]。
Clyclothiazide (100 μM) 使海人酸的剂量反应曲线左移，并导致海人酸在啮齿动物神经元斑块中的 EC50 降低[2]。
Clyclothiazide (100 μM，240 秒) 完全阻断了 3 mM 海人酸在啮齿动物神经元斑块中引起的脱敏作用[2]。
Clyclothiazide (100 μM，3 分钟) 在非洲爪蟾卵母细胞中强烈增强 AMPA 受体反应但对谷氨酸的反应作用较小[3]。
Clyclothiazide (100 μM) 通过亚基调节在 HEK293 中对谷氨酸产生快速脱敏作用细胞[3]。
Clyclothiazide (5 μM，48 小时) 可导致啮齿动物海马神经元出现异常的同步爆发活动，高频动作电位与较大的去极化偏移重叠，并导致神经网络特性的长期变化[4]。
Clyclothiazide (20-50 μM，1-2 小时) 在高浓度下可在啮齿动物海马神经元中短期内引发癫痫样活动[4]。

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

Cyclothiazide 相关抗体:
体内研究
(In Vivo)

Clyclothiazide (Compound CTZ) (1 M，脑室内注射，单剂量) 导致氨基甲酸酯麻醉大鼠自发性复发性癫痫样发作[4]。

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

389.88

同用名

环噻嗪

Formula

C14H16ClN3O4S2
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： 

DMSO 中的溶解度 : 125 mg/mL (320.61 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5649 mL 12.8245 mL 25.6489 mL
5 mM 0.5130 mL 2.5649 mL 5.1298 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。

  • 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

只
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
纯度 & 产品资料

纯度: 98.29%

COA (291 KB) HNMR (337 KB) LCMS (97 KB)

产品使用指南 (1538 KB)
参考文献

Cyclothiazide 相关分类

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
DMSO 1 mM 2.5649 mL 12.8245 mL 25.6489 mL 64.1223 mL
5 mM 0.5130 mL 2.5649 mL 5.1298 mL 12.8245 mL
10 mM 0.2565 mL 1.2824 mL 2.5649 mL 6.4122 mL
15 mM 0.1710 mL 0.8550 mL 1.7099 mL 4.2748 mL
20 mM 0.1282 mL 0.6412 mL 1.2824 mL 3.2061 mL
25 mM 0.1026 mL 0.5130 mL 1.0260 mL 2.5649 mL
30 mM 0.0855 mL 0.4275 mL 0.8550 mL 2.1374 mL
40 mM 0.0641 mL 0.3206 mL 0.6412 mL 1.6031 mL
50 mM 0.0513 mL 0.2565 mL 0.5130 mL 1.2824 mL
60 mM 0.0427 mL 0.2137 mL 0.4275 mL 1.0687 mL
80 mM 0.0321 mL 0.1603 mL 0.3206 mL 0.8015 mL
100 mM 0.0256 mL 0.1282 mL 0.2565 mL 0.6412 mL
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.

Keywords:

Cyclothiazide2259-96-3iGluRGABA ReceptorIonotropic glutamate receptorsGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorAMPA receptor desensitizationpositive allosteric modulatorcurrent potentiationneuronesInhibitorinhibitorinhibit

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