| Bioactivity | PDE4-IN-12 is a potent pan-PDE4 inhibitor, with IC50s of 3.5 and 15 nM for PDE4 and PDE7, respectively (SI=2.71 and 4.27, respectively). PDE4-IN-12 shows well tolerated, can be used in study of inflammatory bowel diseases (IBDs)[1]. |
| Invitro | PDE4-IN-12 (compound 22d) (10, 20 µM; 24 h) reduces the release of NO in LPS induced inflammation cell model (indicates anti-inflammatory effect)[1]. Cell Viability Assay[1] Cell Line: |
| In Vivo | PDE4-IN-12 (5 mg/kg; i.p.; twice daily for 8 days) ameliorates mouse acute colitis induced by DSS (dextran sulfate sodium)[1].PDE4-IN-12 (10 mg/kg; p.o.; single) shows well tolerated in dogs[1].PDE4-IN-1 (2.5 mg/kg; i.v.; single) shows great plasma exposure, with T1/2 and AUC0-24 h values of 4.18 h and 6522 hng/mL[1]. Animal Model: |
| Name | PDE4-IN-12 |
| Formula | C34H35NO6 |
| Molar Mass | 553.64 |
| 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]. Liu H, et al. Discovery of novel PDE4 inhibitors targeting the M-pocket from natural mangostanin with improved safety for the treatment of Inflammatory Bowel Diseases. Eur J Med Chem. 2022 Aug 9;242:114631. |