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  3. GYKI 52466

GYKI 52466 是一种具有口服活性、高选择性和非竞争性的 AMPA/Kainate 受体拮抗剂,其 IC50 值分别为 7.5 和 11 μM。GYKI 52466 具有良好的血脑屏障通透性和抗惊厥作用,可用于帕金森病的研究。

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GYKI 52466 Chemical Structure

GYKI 52466 Chemical Structure

CAS No. : 102771-26-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GYKI 52466 is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 can be used in Parkinson's disease research[1][2].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Neuron IC50
10.8 μM
Compound: GYKI-52466
Inhibition of kainate-induced C57BL/6N mouse hippocampal neurons excitotoxicity after 48 hrs by MTT assay
Inhibition of kainate-induced C57BL/6N mouse hippocampal neurons excitotoxicity after 48 hrs by MTT assay
[PMID: 18083036]
体外研究
(In Vitro)

GYKI 52466 (0.3-100 μM) inhibits inward currents activated by AMPA and Kainate receptor in cultured rat hippocampal neurons[1].

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

体内研究
(In Vivo)

GYKI 52466 (intraperitoneal injection; 1.76-13.2 mg/kg; once) treatment provides potent anticonvulsant protection against sound-induced seizures in DBA/2 mice[2].

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

Animal Model: Male and female DBA/2 mice tested for sound-induced seizure responses[2]
Dosage: 1.76-13.2 mg/kg
Administration: Intraperitoneal injection; 1.76-13.2 mg/kg; once
Result: Observed Maximal anticonvulsant protection after the i.p. treatment (5-15 min ).
分子量

293.32

Formula

C17H15N3O2

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
  • 摩尔计算器

  • 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:
GYKI 52466
目录号:
HY-103234
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