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
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关于此项目
经验公式（希尔记法）:
C14H10BNO3
化学文摘社编号:
分子量:
251.05
NACRES:
NA.77
UNSPSC Code:
12352200
MDL number:
产品名称
Crisaborole, ≥98% (HPLC)
InChI
1S/C14H10BNO3/c16-8-10-1-3-12(4-2-10)19-13-5-6-14-11(7-13)9-18-15(14)17/h1-7,17H,9H2
SMILES string
OB1OCC2=C1C=CC(OC3=CC=C(C#N)C=C3)=C2
InChI key
USZAGAREISWJDP-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 10 mg/mL, clear
storage temp.
room temp
Quality Level
相关类别
Biochem/physiol Actions
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。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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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