1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. GABA Receptor
  3. GABAA receptor agent 7

GABAA receptor agent 7 (compoud 5c) 是一种有效的 GABAA 受体 正调节剂。 GABAA receptor agent 7 在体外和体内均显示出抗惊厥活性且具有低神经毒性。GABAA receptor agent 7 具有癫痫研究潜力。

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GABAA receptor agent 7 Chemical Structure

GABAA receptor agent 7 Chemical Structure

CAS No. : 2376841-18-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GABAA receptor agent 7 (compoud 5c) is a potent GABAA receptor positive modulator. GABAA receptor agent 7 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 7 has the potential for the research of epilepsy[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
0.2 μM
Compound: 5c
Positive allosteric modulation of recombinant human GABA receptor alpha1beta2gamma2 expressed in CHO cells at 30 uM in presence of GABA and measured for 120 secs by FMP dye based FLIPR assay (Rvb = 0.25 +/- 0.03 uM)
Positive allosteric modulation of recombinant human GABA receptor alpha1beta2gamma2 expressed in CHO cells at 30 uM in presence of GABA and measured for 120 secs by FMP dye based FLIPR assay (Rvb = 0.25 +/- 0.03 uM)
[PMID: 31708184]
CHO EC50
3.08 μM
Compound: 5c
Activation of recombinant human GABA receptor alpha1beta2gamma2 expressed in CHO cells in presence of GABA and measured for 120 secs by FMP dye based FLIPR assay
Activation of recombinant human GABA receptor alpha1beta2gamma2 expressed in CHO cells in presence of GABA and measured for 120 secs by FMP dye based FLIPR assay
[PMID: 31708184]
Cortical neurone IC50
0.452 μM
Compound: 5c
Antiepileptic actvity in C57BL/6 mouse Primary cortical neuron assessed as reduction in 4-AP-induced excitability measured for 8 mins by Fluo-8/AM staining based FLIPR assay
Antiepileptic actvity in C57BL/6 mouse Primary cortical neuron assessed as reduction in 4-AP-induced excitability measured for 8 mins by Fluo-8/AM staining based FLIPR assay
[PMID: 31708184]
体外研究
(In Vitro)

GABAA receptor agent 7 (compoud 5c) shows anticonvulsant activity with an IC50 of 0.452 µM in 4-AP induced hyper-excitability Model[1].
GABAA receptor agent 7 (0.01-100 µM; 0-140 s) increases GABA-induced activation of GABAA1 receptor in a dose-dependent manner with EC50 3.08 µM[1].

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

体内研究
(In Vivo)

GABAA receptor agent 7 shows anticonvulsant activity in mice with an ED50 of 31.81 mg/kg and an TD50 of 547.89 mg/kg[1].
GABAA receptor agent 7 specifically attenuates PTZ-induced seizures but not MES-induced seizures in mice[1].

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

分子量

336.78

Formula

C18H13ClN4O

CAS 号
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
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  • 稀释计算器

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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:
GABAA receptor agent 7
目录号:
HY-146099
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