PTUPB|cas:1287761-01-6|西域试剂

PTUPB,98.82%

产品编号：Bellancom-122591| CAS NO：1287761-01-6| 分子式：C₂₆H₂₄F₃N₅O₃S| 分子量：543.56

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货号	价格	库存与货期
Bellancom-122591	￥3500.00	杭州北京（现货）
Bellancom-122591	￥5900.00	杭州北京（现货）
Bellancom-122591	￥11000.00	杭州北京（现货）

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PTUPB

产品介绍

PTUPB 是一种强效的 sEH 和 COX-2 的双向抑制剂，IC₅₀ 值分别为 0.9 nM 和 1.26 μM。

生物活性

PTUPB is a potent and dual sEH and COX-2 enzymes inhibitor with IC₅₀ of 0.9 nM and 1.26 μM, respectively.

体外研究

PTUPB (1-10 μM; 24 hours) shows an inhibitory activity against human 5-LOX, exhibits a 83% and 44% inhibition at 10 μM and 1 μM, respectively.
PTUPB (10-20 μM; 72 hours) has minimal inhibitory effects on cell proliferation in multiple cancer cell lines, including human melanoma cell and a transformed endothelial cell, whereas it potently inhibits HUVEC proliferation after 3 days of application.
PTUPB (10-20 μM; 72 hours) induces cell cycle arrest at the G0/1 phase at different various. The percentage of cell number of PTUPB are 65.15%, 66.87%,and 65.91% at 10 μM, 15 μM, and 20 μM, respectively.

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

Cell Viability Assay

Cell Line:	Multiple cancer cell lines: PC-3 cells, Met-1, H-1, A375, and transformed endothelial cell line (bEnd.3)
Concentration:	10 μM, 15 μM, and 20 μM
Incubation Time:	72 hours
Result:	Inhibited HUVEC proliferation after 3 days.

Cell Cycle Analysis

Cell Line:	HUVECs
Concentration:	10 μM, 15 μM, and 20 μM
Incubation Time:	72 hours
Result:	Induced cell cycle arrest at the G0/1 phase.

体内研究
(In Vivo)

PTUPB (subcutaneous injection; 30 mg/kg; 4 weeks) inhibits LLC tumor growth by 70-83% and exhibits with no overt toxicity, such as any weight loss when it is compared with the control group. After a period of treatment, the peak plasma concentration of PTUPB is high.
PTUPB (subcutaneous injection; 5 mg/kg; once daily; 12 weeks) ameliorates high-fat diet-induced non-alcoholic fatty liver disease via inhibiting NLRP3 inflammasome activation. It reduces body weight, liver weight, liver triglyceride and cholesterol content. It also decreases the expression of lipolytic/lipogenic and lipid uptake related genes.

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

Animal Model:	C57BL/6 mice with LLC cells
Dosage:	30 mg/kg; 4 weeks
Administration:	Subcutaneous injection via Alzet osmotic minipumps; once daily; 4 weeks
Result:	Inhibited LLC tumor growth and metastasis.

Animal Model:	High-fat diet (HFD)-induced obeseadult male C57BL/6 mice
Dosage:	5 mg/kg; 12 weeks
Administration:	Subcutaneous injection; once daily; 12 weeks
Result:	Arrested fibrotic progression and ameliorated high-fat diet-induced non-alcoholic fatty liver disease.

体内研究

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

Animal Model:	C57BL/6 mice with LLC cells
Dosage:	30 mg/kg; 4 weeks
Administration:	Subcutaneous injection via Alzet osmotic minipumps; once daily; 4 weeks
Result:	Inhibited LLC tumor growth and metastasis.

Animal Model:	High-fat diet (HFD)-induced obeseadult male C57BL/6 mice
Dosage:	5 mg/kg; 12 weeks
Administration:	Subcutaneous injection; once daily; 12 weeks
Result:	Arrested fibrotic progression and ameliorated high-fat diet-induced non-alcoholic fatty liver disease.

体内研究

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

Animal Model:	C57BL/6 mice with LLC cells
Dosage:	30 mg/kg; 4 weeks
Administration:	Subcutaneous injection via Alzet osmotic minipumps; once daily; 4 weeks
Result:	Inhibited LLC tumor growth and metastasis.

Animal Model:	High-fat diet (HFD)-induced obeseadult male C57BL/6 mice
Dosage:	5 mg/kg; 12 weeks
Administration:	Subcutaneous injection; once daily; 12 weeks
Result:	Arrested fibrotic progression and ameliorated high-fat diet-induced non-alcoholic fatty liver disease.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (183.97 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8397 mL	9.1986 mL	18.3972 mL
5 mM	0.3679 mL	1.8397 mL	3.6794 mL
10 mM	0.1840 mL	0.9199 mL	1.8397 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 (3.83 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.83 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 (3.83 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.83 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 (3.83 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.83 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。