trans-AUCB 是口服具有活力的、选择性的可溶性环氧水解酶 (sEH) 抑制剂,对人,小鼠和大鼠的 sEH 的IC50分别为 1.3 nM,8 nM,8 nM。它具有抗神经胶质瘤特性。
产品描述
trans-AUCB is an effective and selective soluble epoxide hydrolase inhibitor (IC50s: 1.3 nM, 8 nM, 8 nM for hsEH, mouse sEH and rat sEH, respectively).
体外活性
trans-AUCB (25-300 μM; 48 hours) inhibits U251 and U87 cell growth in a dose-dependent manner. trans-AUCB (200 μM; 48 hours) suppresses U251 and U87 cell growth by activating NF-jB-p65. trans-AUCB (10 μM; 30 min) efficiently suppresses sEH activities in human glioblastoma cell lines and human hepatocellular carcinoma cell lines. trans-AUCB (200 μM; 48 or 96 hours) induces cell-cycle G0/G1 phase arrest in U251 and U87 cells. trans-AUCB (200 μM; 10 min-4 hours) can increase the phosphorylation levels of p65 after 10 min, reaching to peak after 30 min and lasting for at least 2 hours [1].
体内活性
trans-AUCB (i.v.; 0.1 mg/kg) has t1/2 values of 70 min and 10 hours for distribution (α) and elimination (β) phases. trans-AUCB has a CL of 0.7 L/h?kg and a Vdss was 17 L/kg. trans-AUCB (p.o.; 0.1, 0.5, 1 mg/kg) has t1/2 values of 20, 30, 15 min. trans-AUCB (p.o. of 0.1, 0.5, 1 mg/kg) shows Cmax values of 30, 100, 150 nmol/L. trans-AUCB (t-AUCB; p.o.; 0.1, 0.5, 1 mg/kg) ameliorates the LPS-induced hypotension in a dose-dependent manner. trans-AUCB (s.c.; 1, 3, 10 mg/kg) has t1/2 values of 60, 85, 75 min. trans-AUCB(s.c. of 1, 3, 10 mg/kg) has Cmax values of 245, 2700, 3600 nmol/L [2].
Cas No.
885012-33-9
分子式
C24H32N2O4
分子量
412.52
别名
t-AUCB
储存和溶解度
DMSO:100 mg/mL (242.41 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years