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DSR-141562

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Chemical Structure| 2007975-22-4 同义名 : -
CAS号 : 2007975-22-4
货号 : A1327292
分子式 : C19H25F3N4O3
纯度 : 99%+
分子量 : 414.422
MDL号 : N/A
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(60.32 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Cyclic nucleotide phosphodiesterases (PDEs) are enzymes that regulate intracellular signaling by catalyzing the hydrolysis of the second messenger 3’,5’-cAMP and/or 3’,5’-cGMP. DSR-141562 is a novel orally available and brain-penetrant PDE1 inhibitor with an IC50 of 43.9 nM for human PDE1B. DSR-141562 (10 mg/kg; orally) slightly elevated the cGMP concentration, and it potently enhanced the increase of cGMP induced by a dopamine D1 receptor agonist in mouse brains. The cGMP level in monkey cerebrospinal fluid was also elevated after treatment with DSR-141562 at 30 and 100 mg/kg and could be used as a translational biomarker. DSR-141562 (3-30 mg/kg) potently inhibited methamphetamine-induced locomotor hyperactivity in rats. Furthermore, DSR-141562 (0.3-3 mg/kg) reversed social interaction and novel object recognition deficits induced by repeated treatment with an N-methyl-D-aspartate receptor antagonist, phencyclidine, in mice and rats, respectively. In common marmosets, DSR-141562 (3 or 30 mg/kg) improved the performance in object retrieval with detour tasks. These results suggest that DSR-141562 is a therapeutic candidate for positive, negative, and cognitive symptoms in schizophrenia[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.41mL

0.48mL

0.24mL

12.06mL

2.41mL

1.21mL

24.13mL

4.83mL

2.41mL
参考文献

[1]Enomoto T, Tatara A, Goda M, 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. 2019;371(3):692-702. doi:10.1124/jpet.119.260869

[2]Enomoto T, 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. 2019 Dec;371(3):692-702