5.30656

LTA4 Epoxide Hydrolase Inhibitor, ARM1

• Sinonimo/i: LTA4 Epoxide Hydrolase Inhibitor, ARM1, 4-(4-Benzylphenyl)-thiazol-2-amine, Leukotriene A4 Epoxide Hydrolase Inhibitor, LTA₄ Hydrolase Inhibitorq, LTA4H Inhibitor
• Formula empirica (notazione di Hill): C₁₆H₁₄N₂S
• Numero CAS: 68729-05-5
• Peso molecolare: 266.36
• Codice UNSPSC: 12352200
• ID PubChem: 3768902

Proprietà

• Saggio: ≥98% (HPLC)
• Livello qualitativo: 100
• Stato: powder
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: light beige
• Solubilità: DMSO: 100 mg/mL
• Temperatura di conservazione: 2-8°C
• Stringa SMILE: C1=CC=C(C=C1)CC2=CC=C(C=C2)C3=CSC(=N3)N

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
LTA4

Reversible: yes

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

Use only fresh DMSO for reconstitution.

Altre note

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

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable