Comparison

DSR-141562

Item no. CS-0131661-5mg
Manufacturer ChemScene
Amount 5mg
Category
Type Molecules
Specific against other
ECLASS 10.1 32169090
ECLASS 11.0 32169090
UNSPSC 12000000
Alias 2007975-22-4
Similar products 2007975-22-4
Available
CAS
2007975-22-4
Purity
>98%
MWt
414.42
Formula
C19H25F3N4O3
Solubility
DMSO : 50 mg/mL (120.65 mM; Need ultrasonic)
Clinical Information
No Development Reported
Pathway
Metabolic Enzyme/Protease
Target
Phosphodiesterase (PDE)
Biological Activity
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].
Research Area
Neurological Disease

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All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

Amount: 5mg
Available: In stock
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