1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. ITI-214 free base

ITI-214 free base 

Cat. No.: HY-12501 Purity: ≥98.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

ITI-214 free base Chemical Structure

ITI-214 free base Chemical Structure

CAS No. : 1160521-50-5

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5 mg USD 190 In-stock
Estimated Time of Arrival: December 31
10 mg USD 350 Get quote
50 mg USD 950 Get quote
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Description

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].

IC50 & Target[1]

PDE1

58 pM (Ki)

PDE1A

33 pM (Ki)

PDE1B

380 pM (Ki)

PDE1C

35 pM (Ki)

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats[1]
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.
Clinical Trial
Molecular Weight

507.56

Formula

C29H26FN7O

CAS No.
Shipping

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
References
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Product Name:
ITI-214 free base
Cat. No.:
HY-12501
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