AMN082 free base,99.07%
产品编号:Bellancom-103565A| CAS NO:83027-13-8| 分子式:C28H28N2| 分子量:392.54
AMN082自由基是一种选择性、口服活性和脑渗透剂mGluR7激动剂,通过跨膜结构域的变构位点直接激活受体信号。AMN082游离碱基在表达mGluR7的转染哺乳动物细胞上有效抑制cAMP积累并刺激GTPγS结合(EC50值,64-290nm)。AMN082游离碱基显示出对其他mGluR亚型和选择性离子型谷氨酸受体的选择性。抗抑郁作用。
本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,
AMN082 free base
产品介绍 | AMN082 free base 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 free base 有效抑制 cAMP 积累并刺激 GTPγS 结合 (EC50, 64-290 nM)。AMN082 free base 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。 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
生物活性 | AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects. | ||||||||||||||||
体外研究 |
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. 西域 has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||||||
体内研究 |
AMN082 (6 mg/kg; p.o.) induces stress hormone increases in an mGluR7-dependent fashion in mGluR7+/+ mice (C57BL/6 genetic background). 西域 has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||||||
体内研究 |
AMN082 (6 mg/kg; p.o.) induces stress hormone increases in an mGluR7-dependent fashion in mGluR7+/+ mice (C57BL/6 genetic background). 西域 has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||||||
性状 | Solid | ||||||||||||||||
溶解性数据 |
In Vitro:
DMSO : 12.5 mg/mL (31.84 mM; ultrasonic and warming and heat to 60°C) 配制储备液
*
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。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
*以上所有助溶剂都可在 西域 网站选购。
| ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) | ||||||||||||||||
参考文献 |
|
相关文档
化学品安全说明书(MSDS)
下载MSDS质检证书(COA)
相关产品
海关编码 | 2921590090 |
---|
~40% ![]() 83027-13-8 |
文献:Koch, Russell W.; Dessy, Raymond E. Journal of Organic Chemistry, 1982 , vol. 47, # 23 p. 4452 - 4459 |
上游产品 1 | |
---|---|
下游产品 0 |