trans-AUCB - CAS:885012-33-9

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trans-AUCB (Synonyms:t-AUCB)

目录号 : KM9910 CAS No. : 885012-33-9 纯度 : 98%

Data Sheet 产品使用指南

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。

规格	价格	是否有货
1mg		In-stock
5mg		In-stock
10mg		In-stock
50mg	询价	In-stock
100mg	询价	In-stock

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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).

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

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.

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.

分子式

C₂₄H₃₂N₂O₄

分子量

412.52

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。
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。
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。