DSR-141562
- CAS No.
- 2007975-22-4
- Chemical Name:
- DSR-141562
- Synonyms
- DSR-141562;3-methyl-7-(oxan-4-yl)-2-{[(1r,4r)-4-(trifluoromethyl)cyclohexyl]methoxy}-3H,4H-imidazo[4,3-f][1,2,4]triazin-4-one;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;Imidazo[5,1-f][1,2,4]triazin-4(3H)-one, 3-methyl-7-(tetrahydro-2H-pyran-4-yl)-2-[[trans-4-(trifluoromethyl)cyclohexyl]methoxy]-
- CBNumber:
- CB66217789
- Molecular Formula:
- C19H25F3N4O3
- Molecular Weight:
- 414.42
- MDL Number:
- MFCD32701944
- MOL File:
- 2007975-22-4.mol
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P305+P351+P338 |
DSR-141562 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| ChemScene | CS-0131661 | DSR-141562 98.17% | 2007975-22-4 | 5mg | $450 | 2021-12-16 | Buy |
| ChemScene | CS-0131661 | DSR-141562 98.17% | 2007975-22-4 | 10mg | $780 | 2021-12-16 | Buy |
| ChemScene | CS-0131661 | DSR-141562 98.17% | 2007975-22-4 | 50mg | $2300 | 2021-12-16 | Buy |
| ChemScene | CS-0131661 | DSR-141562 98.17% | 2007975-22-4 | 100mg | $3600 | 2021-12-16 | Buy |
DSR-141562 Chemical Properties,Uses,Production
Uses
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].
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. |
IC 50
PDE1
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 DOI:10.1124/jpet.119.260869
[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 of the Japanese Pharmacological Society
DSR-141562 Preparation Products And Raw materials
Raw materials
Preparation Products
DSR-141562 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| Aladdin Scientific | tp@aladdinsci.com | United States | 52924 | 58 | |
| Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696，15000506266 15000506266 | China | 4613 | 55 | |
| Shanghai Chaolan Chemical Technology Center | 021-QQ：65489617 15618227136 | Sales@ATKchemical.com | China | 9342 | 58 |
| Shanghai SuperLan Chemcial Technique Centre | 021-2022843681 15618226720 | lucy@atkchemical.com | China | 10123 | 58 |
| Shanghai Hongye Biotechnology Co. Ltd | 400-9205774 | sales@glpbio.cn | China | 6777 | 58 |
| DC Chemicals | 021-58447131 13564518121 | sales@dcchemicals.com | China | 9409 | 58 |
| ChemeGen(Shanghai) Biotechnology Co.,Ltd. | 18818260767 | sales@chemegen.com | China | 11218 | 58 |
| Bide Pharmatech Ltd. | 400-1647117 13681763483 | product02@bidepharm.com | China | 62072 | 58 |