化合物trans-AUCB T17158

Product Introduction
Bioactivity


英文名: trans-AUCB

描述: trans-AUCB (t-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。

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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 100 mg/mL (242.41 mM)


关键字: epoxide | anti-glioma | transAUCB | hydrolase | activity | orally | sEH | trans AUCB | active | Inhibitor | inhibit | soluble | Epoxide Hydrolase | trans-AUCB

相关产品: EC5026 | CUDA | AR-9281 | VU534 | Valpromide | UC-1728 | PTUPB | GSK2256294A | TPPU | 1,3-Diphenylurea

相关库: NO PAINS Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途