5.30656
LTA4 Epoxide Hydrolase Inhibitor, ARM1
别名:
LTA4 Epoxide Hydrolase Inhibitor, ARM1, 4-(4-Benzylphenyl)-thiazol-2-amine, Leukotriene A4 Epoxide Hydrolase Inhibitor, LTA4 Hydrolase Inhibitorq, LTA4H Inhibitor
SMILES string
C1=CC=C(C=C1)CC2=CC=C(C=C2)C3=CSC(=N3)N
assay
≥98% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
light beige
solubility
DMSO: 100 mg/mL
Quality Level
General description
A cell-permeable benzylphenyl-thiazolamine compound that selectively inhibits against the leukotriene (LT) A4 epoxide hydrolase activity of LTA4H by occupying the same hydrophobic tunnel (Ki = 2.3 µM) targeted by LTA4 ω-end, displaying much reduced potency against LTA4H aminopeptidase activity (% inhibition/[ARM1] = 0/100 µM & 35/1 mM; Substrate = 800 µM Pro-Gly-Pro) coordinated by E296 and the catalytic site Zn2+ at the adjacent hydrophilic peptide substrate-binding cavity. Shown to inhibit A23187- (Cat. Nos. 100105 & 100106) induced LTB4 production in primary human polymorphonuclear neutrophil (PMN) cultures (IC50 = 0.5 µM; ARM1 added 10 min prior to 5 min stimulation by 2.5 µM A23187). Another LTA4H inhibitor SC 57461A (CAS 423169-68-0), in comparison, inhibits both the LTA4-to-LTB4 conversion as well as the chemotactic tripeptide Pro-Gly-Pro degradation activity of LTA4H.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
LTA4
LTA4
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Use only fresh DMSO for reconstitution.
Other Notes
Stsiapanava, A., et al. 2014. Proc. Natl. Acad. Sci. USA111, 4227.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
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