| Name | Crisaborole |
| Description | Crisaborole (AN-2728) is a phosphodiesterase 4 inhibitor. |
| In vitro | AN-2728 inhibits PDE isozymes PDE1A3, PDE3Cat , PDE4Cat and PDE7A1 with IC50 values of 6.1, 6.4, 0.11 and 0.73 μM. AN-2728 inhibits PDE4, TNF-α, IL-2, IFN-γ, IL-5 and IL-10 with IC50 values of 0.49, 0.54, 0.61, 0.83, 2.4 and 5.3 μM. AN-2728 shows the most potent activity against PDE4 catalytic domain, but it also shows inhibition against PDE1A3, PDE3Cat, and PDE7A1. Crystallography reveals that interaction of benzoxaboroles with the hydrophobic pocket in the PDE4 catalytic domain increase their affinity for PDE4. These benzoxaboroles strongly suppresses the secretion of cytokines associated with Ps and AD. |
| In vivo | AN-2728 is well tolerated and significantly impacts efficacy markers, showing comparable results to positive controls in clinical trials. It effectively inhibits ear edema induced by phorbol ester with a dosing of 1 mg/ear×2 (78% and 68%, respectively), mirroring the efficacy of dexamethasone. This suggests AN-2728 possesses notable anti-inflammatory properties and skin penetration capabilities. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 50 mg/mL (199.16 mM)
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| Keywords | Inhibitor | inhibit | AN 2728 | PF06930164 | AN2728 | Crisaborole | PF 06930164 | Phosphodiesterase (PDE) |
| Inhibitors Related | Theobromine | Apremilast | Doxofylline |
| Related Compound Libraries | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | EMA Approved Drug Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Drug Library | Bioactive Compounds Library Max |
United States
