PDE1-IN-4 (compound 2g) 是一种有效且选择性的PDE1(磷酸二酯酶 -1) 抑制剂,其对PDE1C、PDE1A和PDE1B的IC50值分别为 10、145 和 354 nM。PDE1-IN-4 抑制 TGF-β1 诱导的人肺成纤维细胞分化。PDE1-IN-4 通过调控 cAMP (3′,5′- 环磷酸腺苷)和 cGMP (3′,5′- 环磷酸鸟苷)发挥抗纤维化作用。PDE1-IN-4 可用于特发性肺纤维化 (IPF) 研究。
产品描述
PDE1-IN-4 (compound 2g) is a potent and selective PDE1 (phosphodiesterase-1) inhibitor, with IC 50 values of 10, 145, and 354 nM for PDE1C, PDE1A, and PDE1B, respectively. PDE1-IN-4 inhibits myofibroblast differentiation of human lung fibroblasts induced by TGF-β1. PDE1-IN-4 shows anti-fibrosis effects through the regulation of cAMP (3′,5′-cyclic adenosine monophosphate) and cGMP (3′,5′-cyclic guanosine monophosphate). PDE1-IN-4 can be used for idiopathic pulmonary fibrosis (IPF) research [1].
体外活性
PDE1-IN-4 (compound 2g) shows weak inhibition against the hERG channel with an IC 50 above 40 μM, indicating that it will not cause cardiotoxicity [1].
分子式
C33H33N3O4
分子量
535.63
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years