生物活性 |
trans-AUCB (t-AUCB) is a potent, orally active and selectivesolubleepoxide hydrolase(sEH)inhibitor withIC50s of 1.3 nM, 8 nM, 8 nM for hsEH, mouse sEH and rat sEH, respectively. trans-AUCB has anti-glioma activity[1][2].
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IC50& Target |
IC50: 1.3 nM (hsEH), 8 nM (mouse sEH) and 8 nM (rat sEH)[2]
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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].
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. |
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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 t1/2values of 20, 30, 15 min and Cmaxvalues 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 t1/2values of 60, 85, 75 min and Cmaxvalues 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 t1/2values of 70 min and 10 hours for distribution (α) and elimination (β) phases. trans-AUCB has a CL of 0.7 L/hokg and a Vdsswas 17 L/kg[2].
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 t1/2values of 20, 30, 15 min and Cmaxvalues of 30, 100, 150 nmol/L for p.o. of 0.1, 0.5, 1 mg/kg, respectively. |
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分子量 |
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性状 |
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Formula |
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CAS 号 |
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运输条件 |
Room temperature in continental US; may vary elsewhere.
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储存方式 |
Powder |
-20°C |
3 years |
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4°C |
2 years |
In solvent |
-80°C |
6 months |
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-20°C |
1 month |
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溶解性数据 |
In Vitro:
DMSO : 100 mg/mL(242.41 mM;Need ultrasonic)
配制储备液
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 |
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请根据半岛bd体育手机客户端 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半岛bd体育手机客户端 失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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
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1.
请依序添加每种溶剂: 10% DMSO40%PEG3005%Tween-8045% 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。
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2.
请依序添加每种溶剂: 10% DMSO90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。
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3.
请依序添加每种溶剂: 10% DMSO90%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。
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以上所有助溶剂都可在本网站选购。
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