trans-AUCB - 10mM in DMSO , CAS No.885012-33-9

CAS: 885012-33-9 Cat. No.: T655399 分子式: C₂₄H₃₂N₂O₄ 分子量: 412.52 PubChem CID: 16038368

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

概要

trans-AUCB (t-AUCB) is a potent, orally active and selective soluble epoxide hydrolase (sEH) inhibitor with IC 50 s of 1.3 nM, 8 nM, 8 nM for hsEH, mouse sEH and rat sEH, respectively. trans-AUCB has anti-glioma activity

In Vitro

trans-AUCB (t-AUCB; 25-300 μM; 48 hours) suppresses U251 and U87 cell growth in a dose-dependent manner. ?\ntrans-AUCB (200 μM; 48 or 96 hours) induces cell-cycle G0/G1 phase arrest in U251 and U87 cells. ?\ntrans-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. ?\ntrans-AUCB (200 μM; 48 hours) suppresses U251 and U87 cell growth by activating NF-jB-p65. ?\ntrans-AUCB (10 μM; 30 min) efficiently inhibits sEH activities in human glioblastoma cell lines (U251, U87) and human hepatocellular carcinoma cell line (HepG2 cells). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: U251, U87 cells Concentration: 25, 50, 100, 200, or 300 μM Incubation Time: 48 hours Result: Suppressed U251 and U87 cell growth in a dose-dependent manner. Cell Cycle AnalysisCell Line: U251, U87 cells Concentration: 200 μM Incubation Time: 48 or 96 hours Result: Induced cell-cycle G0/G1 phase arrest in U251 and U87 cells. Western Blot AnalysisCell Line: U251, U87 cells Concentration: 200 μM Incubation Time: 10 min, 30 min, 1 hour, 2 hours, or 4 hours Result: Increased the phosphorylation levels of p65 after 10 min, reached to peak after 30 min and lasted for at least 2 hours.

In Vivo

trans-AUCB (t-AUCB; p.o.; 0.1, 0.5, 1 mg/kg) ameliorates the LPS-induced hypotension in a dose-dependent manner. ?\ntrans-AUCB (p.o.; 0.1, 0.5, 1 mg/kg) has t 1/2 values of 20, 30, 15 min and C max values of 30, 100, 150 nmol/L for p.o. of 0.1, 0.5, 1 mg/kg. ?\ntrans-AUCB (s.c.; 1, 3, 10 mg/kg) has t 1/2 values of 60, 85, 75 min and C max values of 245, 2700, 3600 nmol/L for s.c. of 1, 3, 10 mg/kg. ?\ntrans-AUCB (i.v.; 0.1 mg/kg) has t 1/2 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 V dss was 17 L/kg. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Mice (male CFW strain, 7 weeks old, 24-30 g; and male C57BL/6 strain, 8 weeks old, 22-25 g)Dosage: 0.1, 0.5, 1 mg/kg Administration: PO Result: Ameliorated the LPS-induced hypotension in a dose-dependent manner. Animal Model: Mice (male CFW strain, 7 weeks old, 24-30 g; and male C57BL/6 strain, 8 weeks old, 22-25 g)Dosage: 0.1, 0.5, 1 mg/kg (Pharmacokinetic Analysis) Administration: PO Result: Had t 1/2 values of 20, 30, 15 min and C max values of 30, 100, 150 nmol/L for p.o. of 0.1, 0.5, 1 mg/kg, respectively.

IC50& Target:IC50: 1.3 nM (hsEH), 8 nM (mouse sEH) and 8 nM (rat sEH)

Specifications

仕様と純度

10mM in DMSO

生化学的・生理学的メカニズム

trans-AUCB (t-AUCB) is a potent, orally active and selective soluble epoxide hydrolase (sEH) inhibitor with IC 50 s of 1.3 nM, 8 nM, 8 nM for hsEH, mouse sEH and rat sEH, respectively. trans-AUCB has anti-glioma activity.

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

名前と識別子

• 異性体SMILES: C1CC(CCC1NC(=O)NC23CC4CC(C2)CC(C4)C3)OC5=CC=C(C=C5)C(=O)O
• PubChem CID: 16038368
• 分子量: 412.52