trans-AUCB t-AUCB|cas:885012-33-9|西域试剂

trans-AUCB t-AUCB,98.11%

产品编号：Bellancom-113974| CAS NO：885012-33-9| 分子式：C₂₄H₃₂N₂O₄| 分子量：412.52

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货号	价格	库存与货期
Bellancom-113974	￥500.00	杭州北京（现货）
Bellancom-113974	￥1450.00	杭州北京（现货）
Bellancom-113974	￥2550.00	杭州北京（现货）

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trans-AUCB t-AUCB

产品介绍

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。

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.

体外研究

trans-AUCB (t-AUCB; 25-300 μM; 48 hours) suppresses U251 and U87 cell growth in a dose-dependent manner.
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.
trans-AUCB (200 μM; 48 hours) suppresses U251 and U87 cell growth by activating NF-jB-p65.
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).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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

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

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.
trans-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.
trans-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.
trans-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.

西域 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.

体内研究

西域 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.

体内研究

西域 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.

性状

Solid

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。