ITI214 free base

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ITI-214 是一种有效的选择性磷酸二酯酶 1 (PDE1) 抑制剂，Ki 为 58 pM。

ITI-214 is a potent, selective phosphodiesterase 1 (PDE1) inhibitor with Ki of 58 pM, displays >1,000-fold selectivity over PDE4A/4D and other PDE isoforms; improves the memory processes of acquisition, consolidation, and retrieval across a broad dose range (0.1-10 mg/kg, po) without disrupting the antipsychotic-like activity of a clinical antipsychotic medication, shows potential for schizophrenia and Alzheimer's disease, movement disorders, attention deficit and hyperactivity disorders, and other central nervous system (CNS) and non-CNS disorders.Parkinson Disease Phase 2 Clinical.

ITI-214 is found to potently inhibit the activity of full-length recombinant r-hPDE1A (Ki=?34 pM), r-hPDE1B (Ki=?380 pM), and r-hPDE1C (Ki=?37 pM) enzymes transiently expressed in HEK cells. The compound expressed >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.

ITI-214 significantly enhances memory performance in the test with a minimum effective dose of 3 mg/kg. Animal Model:Male Sprague-Dawley ratsDosage: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.

ITI-214 free base | ITI 214 free base

Angiogenesis

PDE

PDE

Neurological Disease

Parkinson Disease

1160521-50-5

507.5614

C29H26FN7O

>98% (HPLC)

10 mM in DMSO

CN1C(=O)C2=C(N(N=C2N3C1=NC4C3CCC4)CC5=CC=C(C=C5)C6=NC(=CC=C6)F)NC7=CC=CC=C7

Cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(2H)-one, 2-[[4-(6-fluoro-2-pyridinyl)phenyl]methyl]-5,6a,7,8,9,9a-hexahydro-5-methyl-3-(phenylamino)-, (6aR,9aS)-

(-20℃)

With Ice Pack

≥ 2 years