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经验配方 C₁₈H₁₆ClN₅O 描述 概述 A cell-permeable pyrazoloquinoline compound that acts as a potent phosphodiesterase 10A inhibitor (Ki≤5 nM against human PDE10A), while exhibiting >500-fold selectivity over other human PDEs 1-11 and little activity against CYP3A4 (IC50 >20 µM) or a panel of 23 kinases (IC50 >30 µM). Reported to be orally available in monkey and rat species and be efficacious in reversing NMDAR antagonist (+)-MK-801- (Cat. No. 475878) induced hyperactivity in a ratsl (MED = 10 mg/kg p.o.) in vivo. 产品目录编号 513050 品牌系列 Calbiochem®
同义词 (6-chloro-3,8-dimethyl-1H-pyrazolo[3,4-b]quinolin-4-yl)(2-methylpyrimidin-5-yl)methanol, Phosphodiesterase 10A Inhibitor 参考 参考 McElroy, W., et al. 2012. Bioorg. Med. Chem. Lett. 22, 1335. 产品信息 形式 Off-white powder Hill配方 C₁₈H₁₆ClN₅O 化学配方 C₁₈H₁₆ClN₅O Molar Mass 353.81 可逆 Y 结构配方图像 生物信息 主靶Ki ≤5 nM 纯度 ≥98% by HPLC 理化信息 细胞可渗透 Y 溶解度 DMSO 储存和货运信息 货运代码 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
毒性 Standard Handling
储存 +2°C to +8°C
避光 Protect from light
无需冷冻 No
特殊指南 Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. 包装信息 惰性气体下包装 Packaged under inert gas
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