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Crisaborole
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Crisaborole图片
CAS NO:906673-24-3
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
AN-2728
PF-06930164
克立硼罗
产品介绍
Crisaborole 是一种有效的 PDE4和cytokine释放抑制剂,能够抑制PDE4(IC50=0.49 μM)。

产品描述

AN-2728 is a Phosphodiesterase 4 Inhibitor.

体外活性

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.

体内活性

AN-2728 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. 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 AN-2728 has good anti-inflammatory activity as well as skin penetration.

Cas No.

906673-24-3

分子式

C14H10BNO3

分子量

251.05

别名

AN-2728;PF-06930164;克立硼罗

储存和溶解度

DMSO:32 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years