5.30656

LTA4 Epoxide Hydrolase Inhibitor, ARM1

• 同義詞: LTA4 Epoxide Hydrolase Inhibitor, ARM1, 4-(4-Benzylphenyl)-thiazol-2-amine, Leukotriene A4 Epoxide Hydrolase Inhibitor, LTA₄ Hydrolase Inhibitorq, LTA4H Inhibitor
• 經驗公式（希爾表示法）: C₁₆H₁₄N₂S
• CAS號碼: 68729-05-5
• 分子量：: 266.36
• 分類程式碼代碼: 12352200
• PubChem物質ID: 3768902

屬性

• 化驗: ≥98% (HPLC)
• 品質等級: 100
• 形狀: powder
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: light beige
• 溶解度: DMSO: 100 mg/mL
• 儲存溫度: 2-8°C
• SMILES 字串: C1=CC=C(C=C1)CC2=CC=C(C=C2)C3=CSC(=N3)N

描述

一般說明

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 (K_i = 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

Reversible: yes

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重構

Use only fresh DMSO for reconstitution.

其他說明

Stsiapanava, A., et al. 2014. Proc. Natl. Acad. Sci. USA111, 4227.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable