1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. DSR-141562

DSR-141562 

Cat. No.: HY-136569 Purity: 98.17%
Handling Instructions

DSR-141562 is a novel, orally active, and selective brain-penetrant phosphodiesterase 1 (PDE1) inhibitor. DSR-141562 shows preferential selectivity for human PDE1B with an IC50 of 43.9 nM, and the IC50 values for human PDE1A and 1C are 97.6 and 431.8 nM, respectively. DSR-141562 can be used for the study of positive symptoms, negative symptoms and cognitive impairments associated with schizophrenia.

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

DSR-141562 Chemical Structure

DSR-141562 Chemical Structure

CAS No. : 2007975-22-4

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5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 780 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2300 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3600 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

DSR-141562 is a novel, orally active, and selective brain-penetrant phosphodiesterase 1 (PDE1) inhibitor. DSR-141562 shows preferential selectivity for human PDE1B with an IC50 of 43.9 nM, and the IC50 values for human PDE1A and 1C are 97.6 and 431.8 nM, respectively. DSR-141562 can be used for the study of positive symptoms, negative symptoms and cognitive impairments associated with schizophrenia[1][2].

IC50 & Target

IC50: 43.9 nM (human PDE1B)
IC50: 97.6 nM (human PDE1A)
IC50: 431.8 nM (human PDE1C)

In Vivo

DSR-141562 (oral administration; 30 mg/kg; single dose; plasma and brain exposures 0.5, 1, 2, and 3 hours after administration) exhibits good brain uptake, with the brain-to-blood concentration ratio of unbound drug being 0.99 in rats.
DSR-141562 (oral administration; 10 mg/kg; single dose; 2 hours) slightly but significantly increases cGMP contents in the frontal cortex and striatum in rat[1].
DSR-141562 (oral administration; 30 mg/kg or 100 mg/kg; single dose; 2 hours) causes a significant increase in cGMP concentration in monkey CSF. The plasma concentrations of unbound this compound are above 43.9 nM (IC50s)for PDE1B in vitro (43.9 nM). DSR-141562 causes a significant increase in cGMP concentration in monkey CSF[1].
DSR-141562 (oral administration; 3 mg/kg, 10 mg/kg and 30 mg/kg; single dose) significantly reverses methamphetamine-induced locomotor hyperactivity, but has no effect on spontaneouslocomotor activity at 3 and 10 mg/kg[1].
DSR-141562 (oral administration; 0.3 mg/kg, 1 mg/kg or 3 mg/kg) significantly reversed the phencyclidine-induced decrease of social interaction time in mice[1].

Animal Model: Male SpragueDawley rats[1]
Dosage: 3 mg/kg, 10 mg/kg and 30 mg/kg
Administration: Oral administration; single dose
Result: Inhibited methamphetamine-induced locomotor hyperactivity in rats, while it had only minimal effects on the spontaneous locomotor activity.
Animal Model: Male SpragueDawley rats[1]
Dosage: 0.3 mg/kg, 1 mg/kg or 3 mg/kg
Administration: Oral administration; single dose
Result: Reversed social interaction.
Molecular Weight

414.42

Formula

C₁₉H₂₅F₃N₄O₃

CAS No.

2007975-22-4

SMILES

O=C1N(C)C(OC[[email protected]]2CC[[email protected]](C(F)(F)F)CC2)=NN3C1=CN=C3C4CCOCC4

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 : 50 mg/mL (120.65 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4130 mL 12.0651 mL 24.1301 mL
5 mM 0.4826 mL 2.4130 mL 4.8260 mL
10 mM 0.2413 mL 1.2065 mL 2.4130 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 (6.03 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution

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

DSR-141562DSR141562DSR 141562Phosphodiesterase (PDE)schizophrenia-relatedsocial interactionlocomotor hyperactivityInhibitorinhibitorinhibit

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