| Bioactivity | PDE4-IN-6 is a potent, safe and moderately selective PDE4 inhibitor with IC50s of 0.125 and 0.43 µM for PDE4B and PDE4D, respectively. PDE4-IN-6 can downregulate the expression level of TNF-α and IL-6. PDE4-IN-6 has potent immunomodulatory activity thereby its potential against rheumatoid arthritis. Anti-inflammatory and anti-arthritic effects[1]. |
| Invitro | PDE4-IN-6 (compound 5f) (0.1-10 µM; 1 hour) has concentration-dependent inhibition on TNF-α in Raw 264.7 cells, with 42.3, 49.6, 57.2 and 68.7% inhibition at concentration of 0.3, 1, 3 and 10 µM[1]. RT-PCR Cell Line: |
| In Vivo | PDE4-IN-6 (10 and 30 mg/kg; i.p.; daily from day 11 until day 20) can improve body weight and reduce paw swelling, also ameliorate joint space narrowing, cartilage degeneration and joint structural deformity in AIA rats at dosing 30 mg/kg[1].PDE4-IN-6 (1-100 μM; incubated 4 days, 3 days or 4 hours) does not induce teratogenicity, hepatotoxicity and cardiac toxicity in zebrafish embryos[1]. Animal Model: |
| Name | PDE4-IN-6 |
| Formula | C25H20FNO5S |
| Molar Mass | 465.49 |
| 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]. Thirupataiah B, et al. Fe(III)-catalyzed regioselective and faster synthesis of isocoumarins with 3-oxoalkyl moiety at C-4: Identification of new inhibitors of PDE4. Bioorg Chem. 2022;121:105667. |