ZD8321

Modify Date: 2024-01-11 13:07:41

ZD8321 Structure
ZD8321 structure
Common Name ZD8321
CAS Number 182073-77-4 Molecular Weight 423.427
Density 1.2±0.1 g/cm3 Boiling Point 573.9±50.0 °C at 760 mmHg
Molecular Formula C18H28F3N3O5 Melting Point N/A
MSDS N/A Flash Point 300.9±30.1 °C

 Use of ZD8321


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

 Names

Name ZD8321
Synonym More Synonyms

 ZD8321 Biological Activity

Description ZD8321 is a potent inhibitor of human Neutrophil elastase (NE) with a Ki of 13±1.7 nM.
Related Catalog
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].
Cell Assay 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.

 Chemical & Physical Properties

Density 1.2±0.1 g/cm3
Boiling Point 573.9±50.0 °C at 760 mmHg
Molecular Formula C18H28F3N3O5
Molecular Weight 423.427
Flash Point 300.9±30.1 °C
Exact Mass 423.198120
LogP 3.26
Vapour Pressure 0.0±1.6 mmHg at 25°C
Index of Refraction 1.471
Storage condition 2-8℃

 Synonyms

T7FIA2S66D
L-Prolinamide, N-(methoxycarbonyl)-L-valyl-N-[(1S)-3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
N-(methoxycarbonyl)-L-valyl-N-[(3S)-1,1,1-trifluoro-4-methyl-2-oxopentan-3-yl]-L-prolinamide
N-(Methoxycarbonyl)-L-valyl-N-[(3S)-1,1,1-trifluoro-4-methyl-2-oxo-3-pentanyl]-L-prolinamide