1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. GABA Receptor
  3. MRK-623

MRK-623 (Compound 14k) 是一种具有口服活性的,高亲和力的 GABAA receptor 激动剂,其对 α1、α2、α3 和 α5 的 Ki 值分别为 0.85 nM、3.7 nM、4.0 nM 和 0.53 nM。MRK-623 显示出抗焦虑的作用。

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MRK-623 Chemical Structure

MRK-623 Chemical Structure

CAS No. : 461449-78-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MRK-623 (Compound 14k) is an orally active, high-affinity GABAA receptor agonist, with the Ki values of 0.85 nM, 3.7 nM, 4.0 nM, and 0.53 nM for α1, α2, α3, and α5, respectively. MRK-623 shows anxiolytic effect[1].

体外研究
(In Vitro)

MRK-623 shows efficacy at human GABAA receptor subtypes expressed in L(tk-) cells measured by whole cell patch-clamp electrophysiology[1].

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

体内研究
(In Vivo)

MRK-623 (oral gavage; 0.3, 1, and 3 mg/kg; once) shows anxiolytic effects in the rat elevated plus maze assay[1].

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

Animal Model: Rat
Dosage: 0.3, 1, and 3 mg/kg
Administration: Oral gavage; 0.3, 1, and 3 mg/kg; once
Result: Showed 78% BZ site occupancy at 3 mg/kg, with an ID50 of 0.8 mg/kg.
分子量

348.37

Formula

C20H17FN4O

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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  • 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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MRK-623
目录号:
HY-123840
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