| Bioactivity | PDE1-IN-4 (compound 2g) is a potent and selective PDE1 (phosphodiesterase-1) inhibitor, with IC50 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]. |
| Invitro | PDE1-IN-4 (compound 2g) shows weak inhibition against the hERG channel with an IC50 above 40 μM, indicating that it will not cause cardiotoxicity[1]. |
| Name | PDE1-IN-4 |
| Formula | C33H33N3O4 |
| Molar Mass | 535.63 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Huang MX, et al. Structural Modifications of Nimodipine Lead to Novel PDE1 Inhibitors with Anti-pulmonary Fibrosis Effects. J Med Chem. 2022 Jun 23;65(12):8444-8455. |