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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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
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 5 mg/mL (18.56 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.7128 mL 18.5639 mL 37.1278 mL
5 mM 0.7426 mL 3.7128 mL 7.4256 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.3%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.7128 mL 18.5639 mL 37.1278 mL 92.8195 mL
5 mM 0.7426 mL 3.7128 mL 7.4256 mL 18.5639 mL
10 mM 0.3713 mL 1.8564 mL 3.7128 mL 9.2819 mL
15 mM 0.2475 mL 1.2376 mL 2.4752 mL 6.1880 mL
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
需求量: