| CAS NO: | 906673-24-3 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| Molecular Weight (MW) | 251.05 |
|---|---|
| Formula | C14H10BNO3 |
| CAS No. | 906673-24-3; 906673-25-4 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: ~50 mg/mL (199.2 mM) |
| Water: N/A | |
| Ethanol: N/A | |
| SMILES | 4-((1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborol-6-yl)oxy)benzonitrile |
| Synonyms | AN-2728; PF06930164; AN 2728; PF-06930164; AN2728; PF 06930164; trade name: Eucrisa |
| SMILES Code | N#CC1=CC=C(OC2=CC=C3C(B(O)OC3)=C2)C=C1 |
| In Vitro | In vitro activity: Crisaborole (AN2728) 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 respectively. Crisaborole exhibits the most potent activity against PDE4 catalytic domain, but it also shows inhibition against PDE1A3, PDE3Cat, and PDE7A1. Crisaborole inhibits PDE isozymes PDE1A3, PDE3Cat , PDE4Cat and PDE7A1 with IC50 values of 6.1, 6.4, 0.11 and 0.73 μM. 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. Crisaborole is a topically administered, boron-containing, anti-inflammatory compound that inhibits PDE4 activity and thereby suppresses the release of TNFalpha, IL-12, IL-23 and other cytokines. Kinase Assay: Crisaborole (AN2728) 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 respectively. Crisaborole exhibits the most potent activity against PDE4 catalytic domain, but it also shows inhibition against PDE1A3, PDE3Cat, and PDE7A1. Crisaborole inhibits PDE isozymes PDE1A3, PDE3Cat , PDE4Cat and PDE7A1 with IC50 values of 6.1, 6.4, 0.11 and 0.73 μM. |
|---|---|
| In Vivo | Crisaborole (AN2728) shows significant inhibition against the ear edema caused by phorbol ester after dosing at 1 mg/ear×2 (78% and 68%, respectively). The efficacy is comparable to that of dexamethasone, suggesting that Crisaborole (AN2728) has good anti-inflammatory activity as well as skin penetration. Crisaborole (AN2728) is reported to be well tolerated and to demonstrate significant effects on markers of efficacy, with results that were comparable to positive controls in clinical trials. |
| Animal model | Male and female (325 each) Crl:CD1(ICR) mice |
| Formulation & Dosage | Formulated in 1% w/v carboxymethylcellulose (CMC); 0, 30, 100, or 300 mg/kg/day; Oral |
| References | J Dermatol Sci. 2017 Aug;87(2):116-122; Curr Opin Investig Drugs. 2009 Nov;10(11):1236-42; Bioorg Med Chem Lett. 2009 Apr 15;19(8):2129-32. |
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