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

ITI-214 

Cat. No.: HY-12501A Purity: 99.57%
Handling Instructions

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.

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

ITI-214 Chemical Structure

ITI-214 Chemical Structure

CAS No. : 1642303-38-5

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 253 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 253 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 190 In-stock
Estimated Time of Arrival: December 31
10 mg USD 350 In-stock
Estimated Time of Arrival: December 31
50 mg USD 950 In-stock
Estimated Time of Arrival: December 31
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200 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

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[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 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[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

605.56

Formula

C₂₉H₂₉FN₇O₅P

CAS No.
SMILES

O=C(C1=C(NC2=CC=CC=C2)N(CC3=CC=C(C4=NC(F)=CC=C4)C=C3)N=C1N56)N(C)C5=N[[email protected]@]7([H])[[email protected]]6([H])CCC7.O=P(O)(O)O

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
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (49.54 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6514 mL 8.2568 mL 16.5136 mL
5 mM 0.3303 mL 1.6514 mL 3.3027 mL
10 mM 0.1651 mL 0.8257 mL 1.6514 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.13 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.13 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.13 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

ITI-214ITI214ITI 214Phosphodiesterase (PDE)motorcognitiveCNS-activeoralselectiveInhibitorinhibitorinhibit

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ITI-214
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HY-12501A
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