A 804598

产品编号: DC9954 Featured
A 804598
结构式
1125758-85-1
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中国地区超过5000个高品质化合物库存
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:
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:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
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:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
产品编号 产品名称 应用领域
DC9954 A 804598 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。
DC7783 AF-353(Ro-4) AF-353 (Ro-4) 是一种有效选择性、口服可利用的 P2X3/P2X2/3 受体拮抗剂, 抑制人和大鼠 P2X3 的 pIC50 值为 8.0,抑制人 P2X2/3 的 pIC50 值为 7.3。