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PTUPB {[allProObj[0].p_purity_real_show]}

货号:A1258087

PTUPB是一种新型的二重 COX2 和 可溶性环氧化酶(sHE)抑制剂。使用 PTUPB 治疗可减少体重、肝脏重量、肝脏甘油三酯和胆固醇含量,以及与脂解/脂合成和脂质摄取相关基因(Acc、Cd36、Cidec)表达,表现出治疗与肥胖相关的肝脏脂肪变性(脂肪肝)的潜力。

PTUPB 化学结构 CAS号:1287761-01-6
PTUPB 化学结构
CAS号:1287761-01-6
PTUPB 3D分子结构
CAS号:1287761-01-6
PTUPB 化学结构 CAS号:1287761-01-6
PTUPB 3D分子结构 CAS号:1287761-01-6
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PTUPB 纯度/质量文件 产品仅供科研

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产品名称 COX COX-1 COX-2 其他靶点 纯度
Piroxicam 98%
Salicylic acid 98%
Phenacetin 98%
Etodolac 99%
Flunixin meglumine 98%
Ibuprofen L-lysine 99%
Nabumetone 98%
Acemetacin 98%
Diflunisal 98%
Pranoprofen 98%
Ampiroxicam 98%
Meloxicam 98%
Sulindac 98%
Ketoprofen 98%
Mefenamic Acid 95%
Bromfenac sodium 98%
Oxaprozin 99%
Aspirin 99%
Nepafenac 98%
Zaltoprofen 99%
Salicin 98%
Suprofen 99%+
Xanthohumol 99%
Parecoxib 98%
Tolfenamic Acid +++

COX-2, IC50: 0.2 μM

98%
Etoricoxib 99%
Niflumic Acid 98%
Valdecoxib ++++

COX-2, IC50: 5 nM

99+%
Ibuprofen +

COX-1, IC50: 13 μM

+

COX-2, IC50: 370 μM

98%
Indomethacin ++

COX1, IC50: 0.28 μM

+

COX-2, IC50: 14 μM

97%
Lornoxicam ++++

COX-1, IC50: 5 nM

++++

COX-2, IC50: 8 nM

98%
Meclofenamic acid sodium ++++

COX-1, IC50: 40 nM

+++

COX-2, IC50: 50 nM

99%
Rofecoxib ++++

COX-2, IC50: 18 nM

98%
Asaraldehyde 98%
Naproxen +

COX-1, IC50: 8.7 μM

+

COX-2, IC50: 5.2 μM

98%
Diclofenac Sodium Salt +++

COX-1, IC50: 60 nM

+++

COX-2, IC50: 200 nM

98%
NS-398 ++

COX-2, IC50: 3.8 μM

95%
Amfenac Sodium Hydrate ++

COX-1, IC50: 250 nM

+++

COX-2, IC50: 150 nM

98%+
Nimesulide +

COX-2, IC50: 26 μM

98%
Lumiracoxib ++

COX-1, Ki: 3 μM

+++

COX-2, Ki: 60 nM

99%
Rutaecarpine 95%
Celecoxib ++++

COX-2, IC50: 40 nM

98%
Carprofen ++++

canine COX2, IC50: 30 nM

98%
Ketorolac ++

COX-1 (human), IC50: 1.23 μM

++

COX-2 (human), IC50: 3.50 μM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

PTUPB 生物活性

描述 PTUPB effectively inhibits both sEH and COX-2 enzymes, demonstrating IC50 values of 0.9 nM and 1.26 μM, respectively[1].
体内研究

PTUPB (subcutaneous injection; 30 mg/kg; 4 weeks) suppresses the growth of LLC tumors by 70-83% without manifesting any significant toxicity, like weight loss, in comparison to the control group. After continuous treatment, the peak concentration of PTUPB in the plasma is observed to be high[1].

PTUPB (subcutaneous injection; 5 mg/kg; once daily; 12 weeks) mitigates non-alcoholic fatty liver disease caused by a high-fat diet through the suppression of NLRP3 inflammasome activation. This treatment leads to a reduction in body and liver weight, as well as decreases in liver triglyceride and cholesterol levels. Furthermore, it lowers the expression of genes associated with lipolysis/lipogenesis and lipid uptake[2].

体外研究

PTUPB (1-10 μM; 24 hours) demonstrates inhibitory effects on human 5-LOX, achieving 83% inhibition at 10 μM and 44% inhibition at 1 μM, respectively[1].

PTUPB (10-20 μM; 72 hours) exerts a slight inhibitory action on the growth of various cancer cell types, such as human melanoma cells and transformed endothelial cells. Yet, it strongly impedes the proliferation of HUVEC cells when applied for a duration of three days[1].

PTUPB (10-20 μM; 72 hours) leads to a halt in the cell cycle at the G0/1 phase at various concentrations. The cell number percentages after PTUPB treatment are 65.15%, 66.87%, and 65.91% for concentrations of 10 μM, 15 μM, and 20 μM, respectively[1].

PTUPB 参考文献

[1]Sun CC, et al. PTUPB ameliorates high-fat diet-induced non-alcoholic fatty liver disease via inhibiting NLRP3 inflammasome activation in mice. Biochem Biophys Res Commun. 2020 Mar 19;523(4):1020-1026.

[2]Zhang G, et al. Dual inhibition of cyclooxygenase-2 and soluble epoxide hydrolase synergistically suppresses primary tumor growth and metastasis. Proc Natl Acad Sci U S A. 2014 Jul 29;111(30):11127-32.

PTUPB 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.84mL

0.37mL

0.18mL

9.20mL

1.84mL

0.92mL

18.40mL

3.68mL

1.84mL

PTUPB 技术信息

CAS号1287761-01-6
分子式C26H24F3N5O3S
分子量 543.561
别名
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place,Inert atmosphere,Room temperature

溶解方案

DMSO: 105 mg/mL(193.17 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案一
方案二
动物实验配方
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