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
方案
≥98% (HPLC)
质量水平
表单
powder
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
light beige
溶解性
DMSO: 100 mg/mL
储存温度
2-8°C
SMILES字符串
C1=CC=C(C=C1)CC2=CC=C(C=C2)C3=CSC(=N3)N
一般描述
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.
生化/生理作用
Cell permeable: yes
Primary Target
LTA4
LTA4
Reversible: yes
包装
Packaged under inert gas
制备说明
Use only fresh DMSO for reconstitution.
其他说明
Stsiapanava, A., et al. 2014. Proc. Natl. Acad. Sci. USA111, 4227.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
Toxicity: Standard Handling (A)
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
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