PZ0037
Crisaborole
≥98% (HPLC), phosphodiesterase 4 (PDE4) inhibitor, powder
别名:
4-[(1,3-二氢-1-羟基-2,1-苯并xaborol-5-基)氧基]苄腈, 5-(4-氰基苯氧基)-1,3-二氢-1-羟基-[2,1]-苯并恶唑, 5-(4-氰基苯氧基)-2,3-二氢-1-羟基-2,1-苯并恶唑, AN2728
生化/生理作用
Crisaborole 是一种非甾体抗炎性磷酸二酯酶 4（PDE4）抑制剂。
Crisaborole 是一种非甾体抗炎性磷酸二酯酶 4（PDE4）抑制剂。Crisaborole 对 PDE4 的 IC50 值为 490 nM，与对释放细胞因子 TNF-α、IL-2 和 IFN-γ 的 IC50 值相似，并且对其他 PDE 同工酶的抑制作用很小。Crisaborole 已被批准作为特应性皮炎的局部治疗方法。
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Chen Dong et al.
The Journal of pharmacology and experimental therapeutics, 358(3), 413-422 (2016-06-30)
Psoriasis and atopic dermatitis are skin diseases affecting millions of patients. Here, we characterize benzoxaborole phosphodiesterase (PDE)-4 inhibitors, a new topical class that has demonstrated therapeutic benefit for psoriasis and atopic dermatitis in phase 2 or phase 3 studies. Crisaborole
Tsutomu Akama et al.
Bioorganic & medicinal chemistry letters, 19(8), 2129-2132 (2009-03-24)
A series of phenoxy benzoxaboroles were synthesized and screened for their inhibitory activity against PDE4 and cytokine release. 5-(4-Cyanophenoxy)-2,3-dihydro-1-hydroxy-2,1-benzoxaborole (AN2728) showed potent activity both in vitro and in vivo. This compound is now in clinical development for the topical treatment
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