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PTUPB
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PTUPB图片
CAS NO:1287761-01-6
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
PTUPB 是一种强效的sEHCOX-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 dualsEHandCOX-2enzymes inhibitor withIC50of 0.9 nM and 1.26 μM, respectively[1].

IC50& Target[2]

COX-2

1.26 μM (IC50)

COX-1

100 μM (IC50)

sEH

0.9 nM (IC50)

体外研究
(In Vitro)

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[1].
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[1].
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[1].

Cell Viability Assay[1]

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[1]

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[1].
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[2].

Animal Model:C57BL/6 mice with LLC cells[1]
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[2]
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.
分子量

543.56

性状

Solid

Formula

C26H24F3N5O3S

CAS 号

1287761-01-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
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 mg5 mg10 mg
1 mM1.8397 mL9.1986 mL18.3972 mL
5 mM0.3679 mL1.8397 mL3.6794 mL
10 mM0.1840 mL0.9199 mL1.8397 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℃, 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

  • 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-CDin 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 μL20% 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。

*以上所有助溶剂都可在本网站选购。