A 438079 hydrochloride CAS号: 899431-18-6分子式: C13H10Cl3N5分子量: 342.61描述纯度储存/保存方法外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
A-438079 hydrochloride is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
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纯度 |
≥98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
外观 |
White to off-white solid
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可溶性/溶解性 |
DMSO : 34.3 mg/mL (100 mM)
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生物活性 | |
靶点 |
P2X7
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In vitro(体外研究) |
In 1321N1 cells stably expressing rat P2X7 receptors, A-438079 blocks BzATP-(10 μM) evoked changes in intracellular calcium concentrations with an IC50 of 321 nM. A-438079 is also selective for the P2X7 receptor, at concentrations up to 100 μM.
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In vivo(体内研究) |
Intraperitoneal injection of A-438079 (5 and 15 mg/kg) 60 min after triggering seizures reduces seizure severity and neuronal death within the hippocampus. A-438079 has superior neuroprotective effects compared with an equally dose of phenobarbital (25 mg/kg). A-438079 partially but significantly prevents the 6-OHDA-induced depletion of striatal DA stores. Pretreatment with A-438079 reduces nociceptive behaviour scores in the HC model. A-438079 (80 μmol/kg, i.v.) reduces noxious and innocuous evoked activity of different classes of spinal neurons in neuropathic rats. A-438079 (100 and 300 μmol/kg, i.p.) significantly raises withdrawal thresh-olds in both the SNL and CCI models.
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分子结构图