ZD8321

目录号: GC32005纯度: >98%

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

Cas No.: 182073-77-4

规格	价格	库存	数量
1mg	¥17,315.00	现货	1
5mg	¥43,197.00	现货	1
10mg	¥73,453.00	现货	1

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187(9):2288-2304 (2024)
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183(7):1867-1883 (2020)
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产品描述 Description

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

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].

[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.

实验参考方法 Experimental Reference Method

Cell experiment:

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].

References:

[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.

产品文档 Product Documents

Purity:>98%

COA SDS Data Sheet

化学性质Chemical Properties

CAS 号

182073-77-4

SMILES

COC(N[C@@H](C(C)C)C(N1[C@@H](CCC1)C(N[C@@H](C(C)C)C(C(F)(F)F)=O)=O)=O)=O

分子式

C₁₈H₂₈F₃N₃O₅

分子量

423.43 g/mol

溶解性

Soluble in DMSO

保存条件

Store at -20°C

General tips

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。

Shipping Condition

评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

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