1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. GABA Receptor
  3. Tiagabine

Tiagabine  (Synonyms: 噻加宾; NO050328; NO328; TGB)

目录号: HY-B0696
产品使用指南

Tiagabine (NO050328) 是一种有效、选择性的 GABA reuptake 抑制剂,为抗惊厥剂;在突触体、神经元和神经胶质中,能够抑制 [3H]GABA 的重摄取,IC50 值分别为 67,446 和 182 nM。

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Tiagabine Chemical Structure

Tiagabine Chemical Structure

CAS No. : 115103-54-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tiagabine (NO050328) is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
> 300 μM
Compound: 1, Tiagabine
Inhibition of [3H]GABA uptake at mouse GAT3 expressed in HEK293 cells after 3 mins by scintillation counting analysis
Inhibition of [3H]GABA uptake at mouse GAT3 expressed in HEK293 cells after 3 mins by scintillation counting analysis
[PMID: 23398473]
HEK293 IC50
> 300 μM
Compound: (R)-1a
Inhibition of mouse mGAT3 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
Inhibition of mouse mGAT3 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
[PMID: 25882526]
HEK293 IC50
0.07 μM
Compound: 5
Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 25 mins by scintillation counting analysis
Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 25 mins by scintillation counting analysis
[PMID: 23336362]
HEK293 IC50
0.64 μM
Compound: 5
Inhibition of rat GAT1 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake by liquid scintillation counting
Inhibition of rat GAT1 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake by liquid scintillation counting
[PMID: 25679268]
HEK293 IC50
0.8 μM
Compound: 1, Tiagabine
Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 3 mins by scintillation counting analysis
Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 3 mins by scintillation counting analysis
[PMID: 23398473]
HEK293 IC50
0.8 μM
Compound: (R)-1a
Inhibition of mouse mGAT1 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
Inhibition of mouse mGAT1 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
[PMID: 25882526]
HEK293 IC50
300 μM
Compound: 1, Tiagabine
Inhibition of [3H]GABA uptake at mouse GAT2 expressed in HEK293 cells after 3 mins by scintillation counting analysis
Inhibition of [3H]GABA uptake at mouse GAT2 expressed in HEK293 cells after 3 mins by scintillation counting analysis
[PMID: 23398473]
HEK293 IC50
300 μM
Compound: (R)-1a
Inhibition of mouse mGAT2 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
Inhibition of mouse mGAT2 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
[PMID: 25882526]
HEK293 IC50
800 μM
Compound: 1, Tiagabine
Inhibition of [3H]GABA uptake at mouse GAT4 expressed in HEK293 cells after 3 mins by scintillation counting analysis
Inhibition of [3H]GABA uptake at mouse GAT4 expressed in HEK293 cells after 3 mins by scintillation counting analysis
[PMID: 23398473]
HEK293 IC50
800 μM
Compound: (R)-1a
Inhibition of mouse mGAT4 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
Inhibition of mouse mGAT4 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis
[PMID: 25882526]
Clinical Trial
分子量

375.55

Formula

C20H25NO2S2

CAS 号
中文名称

噻加宾;替加宾;塞加宾;硫加宾

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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