Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
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.
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].
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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 |
Molecular Formula |
C19H25F3N4O3
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Molecular Weight |
414.4292
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Exact Mass |
414.1879
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Elemental Analysis |
C, 55.07; H, 6.08; F, 13.75; N, 13.52; O, 11.58
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CAS # |
2007975-22-4
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Appearance |
Solid powder
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SMILES |
O=C1N(C)C(OC[C@H]2CC[C@H](C(F)(F)F)CC2)=NN3C1=CN=C3C4CCOCC4
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InChi Key |
LNELWUPBSLZUIQ-MQMHXKEQSA-N
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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-
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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
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Synonyms |
DSR-141562; DSR-141562; DSR141562; DSR141562;; LMN75224; LMN-75224; LMN 75224;
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HS Tariff Code |
2934.99.9001
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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)
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Solubility (In Vitro) |
DMSO : ~25 mg/mL (~60.33 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.03 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.03 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.03 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.