1. GPCR/G Protein Neuronal Signaling
  2. mGluR
  3. ADX71743

ADX71743 是一种高度选择性,非竞争性且透过血脑屏障的代谢型谷氨酸受体 7 负变构调节剂 (mGlu7 NAM)。ADX71743 具有抗焦虑活性。

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ADX71743 Chemical Structure

ADX71743 Chemical Structure

CAS No. : 1431641-29-0

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规格 价格 是否有货 数量
5 mg ¥3383
3 - 4 周
10 mg ¥5416
3 - 4 周
50 mg   询价  
100 mg   询价  

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 has anxiolytic-like activity[1][2].

IC50 & Target[1]

mGlu7

 

体外研究
(In Vitro)

ADX71743 has an IC50 of 300 nM in-house cell lines. Pretreatment of ADX71743 (3 μM; for 20 min) before high-frequency stimulation (HFS) results in an almost complete blockade of LTP induction[1].
ADX71743 (0.1, 10 μM) reverses L-AP4-induced depression of synaptic transmission and results in a concentration-dependent reversal of the L-AP4-induced depression. 0.1 μM ADX71743 reverses the effects of L-AP4 by 11% and 10 μM results in a 20% reversal[2].
ADX71743 can against an EC80 of glutamate (IC50 of 22 nM) as well as against an EC80 of L-AP4 (IC50 of 125 nM)[2].

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

体内研究
(In Vivo)

ADX71743 (50, 100, 150 mg/kg; SC) results in robust reductions in numbers of buried marbles to near maximal levels at lower doses (50 and 100 mg/kg)[2].
ADX71743 (12.5, 100 mg/kg for mice and 100 mg/kg for rat; SC) has a T1/2 of 0.68, 0.40 hours, a Cmax of 1380, 12766 ng/ml of 12.5 mg/kg and 100 mg/kg in mice[2].

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

Animal Model: Adult male C57Bl6/J mice (24-30 g)[2]
Dosage: 50, 100, 150 mg/kg
Administration: SC
Result: Resulted in robust reductions in numbers of buried marbles to near maximal levels at lower doses (50 and 100 mg/kg).
Animal Model: Adult male C57Bl6/J mice (24-30 g) and Sprague-Dawley rats (250-350 g)[2]
Dosage: 12.5, 100 mg/kg for mice and 100 mg/kg for rat (Pharmacokinetic Analysis)
Administration: SC
Result: Had a T1/2 of 0.68, 0.40 hours, a Cmax of 1380, 12766 ng/ml of 12.5 mg/kg and 100 mg/kg in mice.
Had a T1/2 of 1.5 hours, a Cmax of 16800 ng/ml of 100 mg/kg in rat.
分子量

269.34

Formula

C17H19NO2

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

ADX71743 相关分类

  • 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:
ADX71743
目录号:
HY-110278
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