DSR-141562

Cat No.:V2193 Purity: ≥98%
DSR-141562 is a novel, potent, and selective brain-penetrant phosphodiesterase 1 (PDE1) inhibitor.
DSR-141562 Chemical Structure CAS No.: 2007975-22-4
Product category: Phosphodiesterase(PDE)
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

DSR-141562 is a novel, potent, 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. and it is useful for treatment of neurological and psychiatric disorder.

Biological Activity I Assay Protocols (From Reference)
ln Vivo
DSR-141562 (oral; 30 mg/kg; single dose; brain exposure at 0.5, 1, 2, and 3 hours postdose) showed good brain absorption in mice, as evidenced by an unbound drug brain-to-blood concentration ratio of 0.99. within the body. DSR-141562 (single dosage, oral, 10 mg/kg, two hours) cGMP content in the rat frontal cortex and striatum is increased somewhat but noticeably [1]. Monkey CSF cGMP concentrations significantly increased after oral DSR-141562 (30 mg/kg or 100 mg/kg; single dose; 2 hours). The unbound plasma concentration of this drug was more than 43.9 nM (IC50) for PDE1B in vitro (43.9 nM). The quantity of cGMP in monkey CSF fluid is significantly increased by DSR-141562 [1]. At oral dosages of 3 mg/kg, 10 mg/kg, and 30 mg/kg, DSR-141562 (a single dose) dramatically alleviated methamphetamine-induced hyperkinesia, but not locomotor activity. Impact is nonexistent[1]. Mice's deficits in social contact time caused by phencyclidine are considerably reversed by DSR-141562 (oral; 0.3 mg/kg, 1 mg/kg, or 3 mg/kg) [1].
Animal Protocol
Animal/Disease Models: Male Sprague Dawley rat [1]
Doses: 3 mg/kg, 10 mg/kg and 30 mg/kg
Route of Administration: Oral; single dose
Experimental Results: Inhibition of methamphetamine-induced hyperkinesia in rats, but not spontaneous Locomotor activity had only a small effect.

Animal/Disease Models: Male Sprague Dawley rat [1]
Doses: 0.3 mg/kg, 1 mg/kg or 3 mg/kg
Route of Administration: Oral; single dose
Experimental Results: reversal of social interaction.
References
[1]. Takeshi Enomoto, et al.A Novel Phosphodiesterase 1 Inhibitor DSR-141562 Exhibits Efficacies in Animal Models for Positive, Negative, and Cognitive Symptoms Associated With Schizophrenia. J Pharmacol Exp Ther
[2]. Takeshi Enomoto, et al. The Preclinical Profile of DSR-141562: A Novel Phosphodiesterase 1 Inhibitor for the Treatment of Positive Symptoms, Negative Symptoms and Cognitive Impairments Associated with Schizophrenia.Proceedings for The 93rd Annual Meeting
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H25F3N4O3
Molecular Weight
414.4292
Exact Mass
414.1879
CAS #
2007975-22-4
SMILES
O=C1N(C)C(OC[C@H]2CC[C@H](C(F)(F)F)CC2)=NN3C1=CN=C3C4CCOCC4
InChi Key
LNELWUPBSLZUIQ-MQMHXKEQSA-N
InChi Code
InChI=1S/C19H25F3N4O3/c1-25-17(27)15-10-23-16(13-6-8-28-9-7-13)26(15)24-18(25)29-11-12-2-4-14(5-3-12)19(20,21)22/h10,12-14H,2-9,11H2,1H3/t12-,14-
Chemical Name
3-Methyl-7-(tetrahydro-2H-pyran-4-yl)-2-[[trans-4-(trifluoromethyl)cyclohexyl]methoxy]imidazo[5,1-f][1,2,4]triazin-4(3H)-one
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~25 mg/mL (~60.33 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.4130 mL 12.0648 mL 24.1295 mL
5 mM 0.4826 mL 2.4130 mL 4.8259 mL
10 mM 0.2413 mL 1.2065 mL 2.4130 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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