TAK-915 是一种有效的，选择性的，可透过血脑屏障和口服活性的PDE2A抑制剂，IC50为 0.61 nM。TAK-915 对PDE2A的选择性是 PDE1A 的 4100 倍以上。TAK-915 可用于神经精神疾病和神经退行性疾病的研究。
| 生物活性 | TAK-915 is a potent, selective, brain-penetrant and orally activephosphodiesterase2A (PDE2A)inhibitor with anIC50of 0.61 nM. TAK-915 is >4100-fold more selectivity forPDE2Athan PDE1A. TAK-915 has the potential for neuropsychiatric and neurodegenerative disorders treatment[1][2]. |
| IC50& Target[1] | PDE2A 0.61 nM (IC50) | PDE1A 2497 nM (IC50) |
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体内研究
(In Vivo) | TAK-915 (3 mg/kg; oral administration; daily; for 4 days; male F344 rats) treatment significantly reduces escape latency in aged rats in the Morris water maze task[2].
TAK-915 (1, 3, and 10 mg/kg, p.o.) dose-dependently attenuates the non-selective muscarinic antagonist scopolamine-induced memory deficits in rats[2].
Oral dosing of TAK-915 (compound 36) (3 or 10 mg/kg) in mice produces a dose-dependent increase in 3',5'-cyclic guanosine monophosphate (cGMP) levels, with significant cGMP increases observed at a dose of 10 mg/kg[1].
| Animal Model: | Male F344 rats (10-week-old and 26-month-old) bearing morris water maze task[2] | | Dosage: | 3 mg/kg | | Administration: | Oral administration; daily; for 4 days | | Result: | Significantly reduced escape latency in aged rats in the Morris water maze task. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 7.5 mg/mL(16.36 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.1817 mL | 10.9085 mL | 21.8169 mL | | 5 mM | 0.4363 mL | 2.1817 mL | 4.3634 mL | | 10 mM | 0.2182 mL | 1.0908 mL | 2.1817 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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