trans-AUCB(Synonyms: t-AUCB)

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trans-AUCB (Synonyms: t-AUCB) 纯度: 98.11%

trans-AUCB (t-AUCB) 是一种有效的,具有口服活性和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。trans-AUCB 具有抗神经胶质瘤活性。

trans-AUCB(Synonyms: t-AUCB)

trans-AUCB Chemical Structure

CAS No. : 885012-33-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1316 In-stock
1 mg ¥500 In-stock
5 mg ¥1450 In-stock
10 mg ¥2550 In-stock
50 mg   询价  
100 mg   询价  

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trans-AUCB 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Orally Active Compound Library

生物活性

trans-AUCB (t-AUCB) is a potent, orally active and selective soluble epoxide hydrolase (sEH) inhibitor with IC50s of 1.3 nM, 8 nM, 8 nM for hsEH, mouse sEH and rat sEH, respectively. trans-AUCB has anti-glioma activity[1][2].

IC50 & Target

IC50: 1.3 nM (hsEH), 8 nM (mouse sEH) and 8 nM (rat sEH)[2]

体外研究
(In Vitro)

trans-AUCB (t-AUCB; 25-300 μM; 48 hours) suppresses U251 and U87 cell growth in a dose-dependent manner[1].
trans-AUCB (200 μM; 48 or 96 hours) induces cell-cycle G0/G1 phase arrest in U251 and U87 cells[1].
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].
trans-AUCB (200 μM; 48 hours) suppresses U251 and U87 cell growth by activating NF-jB-p65[1].
trans-AUCB (10 μM; 30 min) efficiently inhibits sEH activities in human glioblastoma cell lines (U251, U87) and human hepatocellular carcinoma cell line (HepG2 cells)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell 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 Analysis[1]

Cell 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 Analysis[1]

Cell 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.

体内研究
(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[2].
trans-AUCB (p.o.; 0.1, 0.5, 1 mg/kg) has t1/2 values of 20, 30, 15 min and Cmax values of 30, 100, 150 nmol/L for p.o. of 0.1, 0.5, 1 mg/kg[2].
trans-AUCB (s.c.; 1, 3, 10 mg/kg) has t1/2 values of 60, 85, 75 min and Cmax values of 245, 2700, 3600 nmol/L for s.c. of 1, 3, 10 mg/kg[2].
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[2].

上海金畔生物科技有限公司 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) [2]
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) [2]
Dosage: 0.1, 0.5, 1 mg/kg (Pharmacokinetic Analysis)
Administration: PO
Result: Had t1/2 values of 20, 30, 15 min and Cmax values of 30, 100, 150 nmol/L for p.o. of 0.1, 0.5, 1 mg/kg, respectively.

分子量

412.52

Formula

C24H32N2O4

CAS 号

885012-33-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (242.41 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4241 mL 12.1206 mL 24.2412 mL
5 mM 0.4848 mL 2.4241 mL 4.8482 mL
10 mM 0.2424 mL 1.2121 mL 2.4241 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.04 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.04 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.04 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.04 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.04 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.04 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Li J, et al. t-AUCB, an improved sEH inhibitor, suppresses human glioblastoma cell growth by activatingNF-κB-p65. J Neurooncol. 2012 Jul;108(3):385-93.

    [2]. Liu JY, et al. Pharmacokinetic optimization of four soluble epoxide hydrolase inhibitors for use in a murinemodel of inflammation. Br J Pharmacol. 2009 Jan;156(2):284-96.

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