1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)

ITI214 

Cat. No.: HY-12501A
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.
ITI214 Chemical Structure

ITI214 Chemical Structure

CAS No. : 1642303-38-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO $466 In-stock
5 mg $350 In-stock
10 mg $500 In-stock
50 mg $1500 In-stock
100 mg $2100 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of ITI214:

  • Biological Activity

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  • References

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
NCT Number Sponsor Condition Start Date Phase
NCT01900522 Takeda|Intra-Cellular Therapies, Inc. Schizophrenia July 2013 Phase 1
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References
Molecular Weight

605.56

Formula

C₂₉H₂₉FN₇O₅P

CAS No.

1642303-38-5

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

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 30 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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ITI214
Cat. No.:
HY-12501A
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