1. Metabolic Enzyme/Protease
  2. Elastase
  3. ZD8321

ZD8321 

Cat. No.: HY-U00256 Purity: >95.0%
Handling Instructions

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

For research use only. We do not sell to patients.

ZD8321 Chemical Structure

ZD8321 Chemical Structure

CAS No. : 182073-77-4

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Description

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]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

423.43

Formula

C₁₈H₂₈F₃N₃O₅

CAS No.

182073-77-4

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
References
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

ZD8321ZD 8321ZD-8321ElastaseInhibitorinhibitorinhibit

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