ZD8321

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ZD8321 

ZD8321 是人 Neutrophil elastase (NE) 的有效抑制剂，其 Ki 值为 13±1.7 nM。

ZD8321

ZD8321 Chemical Structure

CAS No. : 182073-77-4

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生物活性

ZD8321 is a potent inhibitor of human Neutrophil elastase (NE) with a Ki of 13±1.7 nM.

IC50 & Target

Ki: 13±1.7 nM (Neutrophil elastase)[1]
体外研究
(In Vitro)

TNFα-activated HUVEC is dose dependently inhibited by ZD8321.The adhesion between cancer cells with high elastase activity and TNFα-activated HUVEC is also inhibited by ZD8321. Expression of cell surface E-selectin by NE stimulation is suppressed in the presence of ZD8321. The concentration of soluble E-selectin in the medium increases after adhesive reaction between neutrophils and HUVEC. This increase is also dose dependently inhibited by ZD8321[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

423.43

Formula

C18H28F3N3O5
CAS 号

182073-77-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [1]. Veale CA, et al. Orally active trifluoromethyl ketone inhibitors of human leukocyte elastase. J Med Chem. 1997 Sep 26;40(20):3173-81.

    [2]. Nozawa F, et al. Elastase activity enhances the adhesion of neutrophil and cancer cells to vascular endothelial cells. J Surg Res. 2000 Dec;94(2):153-8.
Cell Assay
[2]

HUVECs are cultured in RPMI 1640 containing 5% FBS for 6 h in collagen-coated, 24-well plates before the experiment. Some of the confluent HUVECs are further incubated with TNFα (1 ng/mL) and ZD8321 (0-50 mM), or with human NE (0-100ng/mL) for 4 h at 37°C. For adhesion assays, cancer cells resuspended in RPMI 1640 containing 5% FBS are added to each HUVEC-layered well. The plates are shaken at 700 rpm for 10 min at room temperature, washed twice with PBS, and examined by phase-contrast microscopy to determine the number of cells bound onto the HUVEC monolayer. The adhesive reactions of neutrophils to HUVEC are also analyzed in this manner[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Veale CA, et al. Orally active trifluoromethyl ketone inhibitors of human leukocyte elastase. J Med Chem. 1997 Sep 26;40(20):3173-81.

    [2]. Nozawa F, et al. Elastase activity enhances the adhesion of neutrophil and cancer cells to vascular endothelial cells. J Surg Res. 2000 Dec;94(2):153-8.

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