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PDE1-IN-4
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PDE1-IN-4图片

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PDE1CPDE1APDE1BIC50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。
生物活性

PDE1-IN-4 (compound 2g) is a potent and selectivePDE1(phosphodiesterase-1) inhibitor, withIC50values of 10, 145, and 354 nM forPDE1C,PDE1A, andPDE1B, respectively. PDE1-IN-4 inhibits myofibroblast differentiation of human lung fibroblasts induced byTGF-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].

IC50& Target

PDE1C

10 ± 3 nM (IC50)

PDE1A

145 nM (IC50)

PDE1B

354 nM (IC50)

PDE4B2

619 nM (IC50)

PDE4D2

948 nM (IC50)

PDE10A

1310 nM (IC50)

PDE5A1

1810 nM (IC50)

PDE2A

5130 nM (IC50)

PDE3A

>10000 nM (IC50)

PDE9A2

>10000 nM (IC50)

体外研究
(In Vitro)

PDE1-IN-4 (compound 2g) shows weak inhibition against the hERG channel with an IC50above 40 μM, indicating that it will not cause cardiotoxicity[1].

分子量

535.63

Formula

C33H33N3O4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

 
 
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