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- 产品描述： ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions
- 靶点： PDE1:58 pM (Ki);PDE1A:33 pM (Ki);PDE1B:380 pM (Ki);PDE1C:35 pM (Ki)
- 体外研究： ITI-214 expresses >1000-fold greater activity toward PDE1 isoforms compared with the next nearest PDE family enzyme, PDE4D (Ki= 33 nM) and 10,000-300,000-fold selectivity toward all other PDE enzyme families
- 体内研究： ITI-214 significantly enhances memory performance in the test with a minimum effective dose of 3 mg/kg. Animal Model: Male Sprague-Dawley rats Dosage: 0.1-10 mg/kg Administration: p.o. Result: Significantly enhanced memory performance in the test with a minimum effective dose of 3 mg/kg.
- 参考文献：
1. Li P, et al. Discovery of Potent and Selective Inhibitors of Phosphodiesterase 1 for the Treatment of Cognitive Impairment Associated with Neurodegenerative and Neuropsychiatric Diseases. J Med Chem. 2016;59(3):1149-1164. 2. Snyder GL, et al. Preclinical profile of ITI-214, an inhibitor of phosphodiesterase 1, for enhancement of memory performance in rats. Psychopharmacology (Berl). 2016;233(17):3113-3124.
- 溶解性： soluble in DMSO
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 1.651 ml 8.257 ml 16.514 ml 5 mM 0.33 ml 1.651 ml 3.303 ml 10 mM 0.165 ml 0.826 ml 1.651 ml 50 mM 0.033 ml 0.165 ml 0.33 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
