产品
编 号：F514247
分子式：C14H10BNO3
分子量：251.05
分子式：C14H10BNO3
分子量：251.05
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
112
In-stock
5mg
225
In-stock
10mg
360
In-stock
50mg
560
In-stock
100mg
760
In-stock
结构图
CAS No: 906673-24-3
产品详情
生物活性：
Crisaborole (AN-2728) is a potent inhibitor of PDE4 and cytokine release; inhibit PDE4 with an IC50 of 0.49 μM.
体内研究：
Crisaborole (AN-2728) 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 (AN-2728) has good anti-inflammatory activity as well as skin penetration. Crisaborole (AN-2728) is reported to be well tolerated and to demonstrate significant effects on markers of efficacy, with results that are comparable to positive controls in clinical trials.
体外研究：
Crisaborole (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. Crisaborole (AN-2728) shows the most potent activity against PDE4 catalytic domain, but it also shows inhibition against PDE1A3, PDE3Cat, and PDE7A1. Crisaborole (AN-2728) 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 (AN-2728) 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.
Crisaborole (AN-2728) is a potent inhibitor of PDE4 and cytokine release; inhibit PDE4 with an IC50 of 0.49 μM.
体内研究：
Crisaborole (AN-2728) 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 (AN-2728) has good anti-inflammatory activity as well as skin penetration. Crisaborole (AN-2728) is reported to be well tolerated and to demonstrate significant effects on markers of efficacy, with results that are comparable to positive controls in clinical trials.
体外研究：
Crisaborole (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. Crisaborole (AN-2728) shows the most potent activity against PDE4 catalytic domain, but it also shows inhibition against PDE1A3, PDE3Cat, and PDE7A1. Crisaborole (AN-2728) 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 (AN-2728) 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.
产品资料
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