A 804598
产品编号: DC9954
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应用领域
A-804598 是一个 CNS 渗透,竞争性和选择性的 P2X7 受体拮抗剂,作用于小鼠,大鼠和人的 P2X7 受体,IC50s 分别是 9 nM, 10 nM 和 11 nM。
Cas No.: |
1125758-85-1 |
名称: |
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别名: |
A 804598; A804598 |
SMILES: |
CC1=CC(C(CN2C(CCC2=O)=O)=O)=C(N1CC3=CC=CC=C3)C |
分子式: |
C19H12N6 |
分子量: |
315.37 |
纯度: |
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保存条件: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: |
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In Vivo: |
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In Vitro: |
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References: |
A-804598 is a novel, competitive, and selective P2X7 receptor antagonist with IC50 of 10 nM, 9 nM and 11 nM in rat, mouse and human P2X7 receptors respectively.
In vitro: A-804598 potently blocked IL-1β release in the THP-1 cells (IC50 of 8.5 nM). A-804598 also blocked agonist-evoked pore formation in differentiated human THP-1 cells (IC50 of 8.1 nM) with similar potency as in the calcium-influx assay.In vivo: Autoradiographic analysis of coronal rat brain sections revealed that there was specific binding of [3H]-A-804598 throughout the rat brain. High levels of [3H]-A-804598 specific binding were also found in the grey matter of the L4-L6 region of the rat spinal cord. |
Kinase Assay: |
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Cell Assay: |
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Animal Administration: |
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References: |
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MSDS
COA
LOT NO. |
DOWNLOAD |
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2018-0101 |
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