1. GPCR/G Protein Neuronal Signaling Apoptosis
  2. mGluR Apoptosis
  3. Fenobam hydrate

Fenobam hydrate 是一种具有选择性和口服活性的 mGluR5 拮抗剂 (IC50=84 nM),能穿过血脑屏障。Fenobam hydrate 在大鼠和人重组 mGlu5 受体上的 Kd 值分别 54 nM 和 31 nM。Fenobam hydrate 具有抗焦虑活性,能抑制大鼠的自我给药行为,还可诱导癌细胞凋亡 (apoptosis)。Fenobam hydrate 可用于神经系统疾病、癌症以及药物成瘾的研究。

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Fenobam hydrate Chemical Structure

Fenobam hydrate Chemical Structure

CAS No. : 63540-28-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Fenobam hydrate is a selective and orally active mGluR5 antagonist (IC50=84 nM) that can penetrate the blood-brain barrier. Fenobam hydrate shows the Kd values of 54 nM and 31 nM on rat and human recombinant mGlu5 receptors, respectively. Fenobam hydrate has anxiolytic activity, inhibits self-administration behavior in rat, and induces apoptosis in cancer cells. Fenobam hydrate can be used for research on neurological diseases, cancer and drug addiction[1][2][3].

IC50 & Target[1]

mGluR5

84 nM (IC50)

human mGluR5

31 nM (Kd)

rat mGluR5

54 nM (Kd)

体外研究
(In Vitro)

Fenobam hydrate (300 μM; 72 h) 显著抑制 LM7 细胞的增殖,并诱导细胞凋亡[2]

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

Apoptosis Analysis[2]

Cell Line: LM7 cells
Concentration: 300 μM
Incubation Time: 72 h
Result: Significantly reduced total number of cells, proliferating cells, and induced apoptosis.
体内研究
(In Vivo)

Fenobam hydrate (30-60 mg/kg; p.o.; 3 times a week) 显著抑制大鼠的自我给药行为[3]

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

Animal Model: Male Long-Evans rats (250-300 g)[3].
Dosage: 30-60 mg/kg
Administration: Oral administration; 3 times a week.
Result: Inhibited self-administration.
分子量

284.70

Formula

C11H13ClN4O3

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:
Fenobam hydrate
目录号:
HY-101478A
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