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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Phosphodiesterase (PDE)-IMR-687
IMR-687

Chemical Structure : IMR-687

CAS No.: 2062661-53-2

IMR-687 (IMR687, Tovinontrine)

货号: PC-72172Not For Human Use, Lab Use Only.

IMR-687 (IMR687, Tovinontrine) is a novel, potent and selective phosphodiesterase-9 (PDE-9) inhibitor with IC50 of 8.19 nM and 9.99 nM against PDE9A1 and PDE9A2, respectively.

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

生物&药学活性

IMR-687 (IMR687, Tovinontrine) is a novel, potent and selective phosphodiesterase-9 (PDE-9) inhibitor with IC50 of 8.19 nM and 9.99 nM against PDE9A1 and PDE9A2, respectively.
IMR-687 (Tovinontrine) displays>800-fold greater potency than PDE1A3, PDE1B, PDE1C, PDE5A2 (IC50 values >8 uM).
IMR-687 (Tovinontrine) recapitulates the cGMP and fetal hemoglobin (HbF) induction mechanism of hydroxyurea (HU) in erythroid cells.
Treatment of phosphodiesterase 9A inhibitor (IMR-687, Tovinontrine) in sickle mice for 30 days results in fetal hemoglobin (HbF) induction, reduced hemolysis and reticulocytosis, as well as immune cell activity.
IMR-687 (Tovinontrine) increases F-cells in patient-derived sickle cell disease (SCD) CD36+ cells, reduces vessel-occlusion in the Townes-HbSS sickle cell disease model.

物理化学性质&存储条件

分子量 394.479
分子式 C21H26N6O2
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

6-{(3S,4S)-4-methyl-1-[(pyrimidin-2-yl)methyl]pyrrolidin-3-yl}-3-(oxan-4-yl)imidazo[1,5-a]pyrazin-8(7H)-one

参考文献

1. McArthur JG, et al. Haematologica. 2020 Mar;105(3):623-631.

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