ITI-214 free base_product_DataBase

Bioactivity

ITI-214 free base 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 free base inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 free base shows efficacy in various animal models of motor and cognitive functions[1][2].

Invitro

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[2].

In Vivo

ITI-214 significantly enhances memory performance in the test with a minimum effective dose of 3 mg/kg[1]. Animal Model:

Name

ITI-214 free base

CAS

1160521-50-5

Formula

C29H26FN7O

Molar Mass

507.56

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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 Feb 11;59(3):1149-64. [2]. Lawrence Wennogle. Novel uses. From PCT Int. Appl. (2014), WO 2014145617 A2 20140918. [3]. Peng Li , et al. Salt crystals. From PCT Int. Appl. (2013), WO 2013192556 A2 20131227. [4]. Allen A. Fienberg, et al. Organic compounds. From PCT Int. Appl. (2010), WO 2010132127 A1 20101118.

PeptideDB

ITI-214 free base

CAS: 1160521-50-5 F: C29H26FN7O W: 507.56