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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Phosphodiesterase (PDE)-DSR-141562
DSR-141562

Chemical Structure : DSR-141562

CAS No.: 2007975-22-4

DSR-141562 (DSR141562)

货号: PC-47111Not For Human Use, Lab Use Only.

DSR-141562 (DSR141562) is a potent, selective orally available and brain-penetrant phosphodiesterase 1 (PDE1) inhibitor with IC50 of 97.6, 43.9 and 431.8 nM for human PDE1A, PDE1B and PDE1C, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

DSR-141562 (DSR141562) is a potent, selective orally available and brain-penetrant phosphodiesterase 1 (PDE1) inhibitor with IC50 of 97.6, 43.9 and 431.8 nM for human PDE1A, PDE1B and PDE1C, respectively.
DSR-141562 shows 2.2- and 9.8-fold selectivity for PDE1B over PDE1A and PDE1C, but has no effect or only weak inhibitory effects for other PDE families (PDE2A, IC50=2480 nM).
DSR-141562 elevated the tissue level of cGMP in mouse striatum and frontal cortex, as well as cGMP level in the monkey CSF.
DSR-141562 demonstrated efficacy in animal models for schizophrenia, DSR-141562 (3–30 mg/kg) inhibited methamphetamine-induced locomotor hyperactivity in rats.

物理化学性质&存储条件

分子量 414.429
分子式 C19H25F3N4O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

参考文献

1. Enomoto T, et al. J Pharmacol Exp Ther. 2019 Dec;371(3):692-702.

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