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 picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).

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

ITI-214 Chemical Structure

ITI-214 Chemical Structure

CAS No. : 1642303-38-5

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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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Based on 1 publication(s) in Google Scholar

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Description

ITI-214 is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM). IC50 value: 58 pM (Ki) Target: PDE1 in vitro: ITI-214 exhibits picomolar inhibitory potency for PDE1, demonstrates excellent selectivity against all other PDE families. ITI214 exhibits excellent selectivity over other PDE family members. For instance, the Ki values of ITI214 against recombinant full-length human PDE1A, PDE1B, and PDE1C are 33 pM, 380 pM, and 35 pM, respectively. ITI214 is profiled in a panel of enzymes, receptors, transporters, and ion channels from Caliper at 10 μM, which is over 170000 times higher than its Ki for PDE1, and demonstrates good selectivity. [1] in vivo: ITI214 possesses a good overall profile with balanced physicochemical properties, excellent potency and selectivity, and good pharmacokinetics. ITI214 is found to significantly enhance memory performance in the test with a minimum effective dose of 3 mg/kg. [1]

Clinical Trial
Molecular Weight

605.56

Formula

C₂₉H₂₉FN₇O₅P

CAS No.

1642303-38-5

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)Inhibitorinhibitorinhibit

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ITI-214
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HY-12501A
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