Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: N''-[N-METHOXYCARBONYL-L-VALYL]-N-[(S)-3,3,3-TRIFLUOR-1-ISOPROPYL-2-OXOPROPYL]-L-PROLINAMIDE
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Purity: 98.0%
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182073-77-4

182073-77-4 structure

182073-77-4 structure

Name: ZD8321
Chemical Name: ZD8321
CAS Number: 182073-77-4
Molecular Formula: C₁₈H₂₈F₃N₃O₅
Molecular Weight: 423.427
Catalog: Signaling Pathways Metabolic Enzyme/Protease Elastase
Create Date: 2018-04-11 02:08:30
Modify Date: 2024-01-11 13:07:41
ZD8321 is a potent inhibitor of human Neutrophil elastase (NE) with a Ki of 13±1.7 nM.

Name	ZD8321
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

Description	ZD8321 is a potent inhibitor of human Neutrophil elastase (NE) with a Ki of 13±1.7 nM.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Elastase Research Areas >> Cancer Research Areas >> Inflammation/Immunology
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.

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℃