1. GPCR/G Protein Neuronal Signaling
  2. mGluR
  3. AMN082

AMN082 是一种选择性,具有口服活性,可透过血脑屏障的 mGluR7 激动剂,通过跨膜区的变构位点直接激活受体信号。在表达 mGluR7 的转染哺乳动物细胞上,AMN082 有效抑制 cAMP 积累并刺激 GTPγS 结合 (EC50, 64-290 nM)。AMN082 对其他 mGluR 亚型和选择性离子型谷氨酸受体具有选择性。具有抗抑郁作用。

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AMN082 Chemical Structure

AMN082 Chemical Structure

CAS No. : 97075-46-2

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规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1741
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1 mg ¥647
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5 mg ¥1700
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10 mg ¥2800
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25 mg ¥5800
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50 mg ¥9300
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Customer Review

Other Forms of AMN082:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects[1][2].

体外研究
(In Vitro)

Preincubation of the synaptosomes with AMN082 (1 μM) for 10 min before 4-aminopyridine treatment efficiently inhibits the 4-aminopyridine-evoked release of glutamate, without altering the basal release of glutamate[2].

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

体内研究
(In Vivo)

AMN082 (6 mg/kg; p.o.) induces stress hormone increases in an mGluR7-dependent fashion in mGluR7+/+ mice (C57BL/6 genetic background)[1].
AMN082 (1.25-5.0 mg/kg, i.p.; 30 min before every Cocaine or Morphine injection during repeated drug administration or before Cocaine or Morphine challenge) dose-dependently attenuates the development, as well as the expression of Cocaine or Morphine locomotor sensitization[3].

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

Animal Model: Male Swiss mice (20-25g)[3]
Dosage: 1.25, 2.5, 5.0 mg/kg
Administration: I.p.; given 30 min prior to Cocaine (10 mg/kg) or Morphine (10 mg/kg) challenge on day 17 or 20, respectively
Result: Significantly attenuated the expression of Cocaine-induced locomotor sensitization; Attenuated the induction of Morphine-induced sensitization.
分子量

465.46

Formula

C28H30Cl2N2

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
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 33.33 mg/mL (71.61 mM; 超声助溶; 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 2.1484 mL 10.7421 mL 21.4841 mL
5 mM 0.4297 mL 2.1484 mL 4.2968 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
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 2.1484 mL 10.7421 mL 21.4841 mL 53.7103 mL
5 mM 0.4297 mL 2.1484 mL 4.2968 mL 10.7421 mL
10 mM 0.2148 mL 1.0742 mL 2.1484 mL 5.3710 mL
15 mM 0.1432 mL 0.7161 mL 1.4323 mL 3.5807 mL
20 mM 0.1074 mL 0.5371 mL 1.0742 mL 2.6855 mL
25 mM 0.0859 mL 0.4297 mL 0.8594 mL 2.1484 mL
30 mM 0.0716 mL 0.3581 mL 0.7161 mL 1.7903 mL
40 mM 0.0537 mL 0.2686 mL 0.5371 mL 1.3428 mL
50 mM 0.0430 mL 0.2148 mL 0.4297 mL 1.0742 mL
60 mM 0.0358 mL 0.1790 mL 0.3581 mL 0.8952 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:
AMN082
目录号:
HY-103565
需求量: