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| 品牌 | absin | CAS | 899431-18-6 |
|---|---|---|---|
| 分子式 | C13H10Cl3N5 | 纯度 | ≥98% |
| 分子量 | 342.61 | 货号 | abs47028127 |
| 规格 | 10mg | 供货周期 | 现货 |
| 主要用途 | is a potent, and selective P2X7 receptor | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
A 438079 hydrochloride 899431-18-6
| 产品描述 | |
| 描述 | A-438079 hydrochloride is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9. |
| 纯度 | ≥98% |
| 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. |
| 基本信息 | |
| 外观 | White to off-white solid |
| 可溶性/溶解性 | DMSO : 34.3 mg/mL (100 mM) |
| 生物活性 | |
| 靶点 | P2X7 |
| 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. |
| 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. |
| 研究领域 | |
| 研究领域 | NeuroscienceProcesses NeuroscienceNeurotransmissionReceptors / ChannelsLigand-Gated Ion ChannelsP2X Receptors Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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