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别名 PF-2545920
Mardepodect (PF-2545920) 是一种有效的、口服具有活性的、可透过血脑屏障的、选择性的 PDE10A 抑制剂,IC50=0.37 nM,比作用于其他 PDE 选择性高 1000 多倍。

Mardepodect (PF-2545920) 是一种有效的、口服具有活性的、可透过血脑屏障的、选择性的 PDE10A 抑制剂,IC50=0.37 nM,比作用于其他 PDE 选择性高 1000 多倍。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 413 | 现货 | |
| 5 mg | ¥ 826 | 现货 | |
| 10 mg | ¥ 1,320 | 现货 | |
| 25 mg | ¥ 2,490 | 现货 | |
| 50 mg | ¥ 3,930 | 现货 | |
| 100 mg | ¥ 5,730 | 现货 | |
| 200 mg | ¥ 7,750 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 890 | 现货 |
| 产品描述 | Mardepodect (PF-2545920) is a phosphodiesterase inhibitor selective for the PDE10A subtype with an IC50 of 0.37 nM, >1000-fold selectivity over PDE. It is potentially useful for the treatment of schizophrenia. Phosphodiesterase 10A (PDE10A) is highly expressed in striatal medium spiny neurons of both the direct and indirect output pathways. Mardepodect can cross the blood-brain barrier. |
| 靶点活性 | PDE10A:0.37 nM |
| 体内活性 | Mardepodect is active in a range of antipsychotic models with the ED50 of 1 mg/kg, antagonizing apomorphine-induced climbing in mice, inhibiting conditioned avoidance responding in both rats and mice, and blocking N-methyl-D-aspartate antagonist-induced deficits in prepulse inhibition of acoustic startle response in rats, while improving baseline sensory gating in mice.Mardepodect induces a dose-dependent increase in striatal cGMP in mice. |
| 别名 | PF-2545920 |
| 分子量 | 392.45 |
| 分子式 | C25H20N4O |
| CAS No. | 898562-94-2 |
| Smiles | Cn1cc(c(n1)-c1ccc(OCc2ccc3ccccc3n2)cc1)-c1ccncc1 |
| 密度 | 1.31g/cm3 |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 45 mg/mL (114.66 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.1 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。
对于不同动物的给药剂量换算,您也可以参考 更多