Mardepodect

产品编号 T16499Cas号 898562-94-2

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。

产品编号 T16499别名 PF-2545920Cas号 898562-94-2

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。

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生物活性

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

化学信息

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

DMSO: 45 mg/mL (114.66 mM)

溶液配制表

DMSO