ITI-214 phosphate is an orally active, potent and selective inhibitors of PDE1, exhibits potent PDE1 inhibitory activity (Ki = 58 pM). ITI-214 demonstrated excellent selectivity against all other PDE families.
ITI-214 showed good efficacy in vivo, it is found to significantly enhance memory performance in the test with a minimum effective dose of 3 mg/kg.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO ≥ 15 mg/mL|
Discovery of Potent and Selective Inhibitors of Phosphodiesterase 1 for the Treatment of Cognitive Impairment Associated with Neurodegenerative and Neuropsychiatric Diseases.
Li P, et al. J Med Chem. 2016 Feb 11;59(3):1149-64. PMID: 26789933.
|Related PDE Products|
CP671305 is a potent and selective, orally active inhibitor of phosphodiesterase-4-D with high activities.
IBMX is a pDE inhibitor (non-selective) with IC50 values of 6.5±1.2, 26.3±3.9 and 31.7±5.3 μM for PDE3, 4 and 5 respectively.
GLPG1690 (Ziritaxestat) is a first-in-class autotaxin (ATX) inhibitor, with IC50 of 131 nM and Ki of 15 nM.
RVT-501 (E6005) is a selective phosphodiesterase 4 (PDE4PDE4) inhibitor with an IC50 of 2.8 nM.
Vardenafil Hcl is a PDE5 inhibitor used for treating erectile dysfunction.
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