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PTUPB {[allProObj[0].p_purity_real_show]}

货号:A1258087 Ambeed 开学季,买赠积分,赢豪礼

PTUPB is a novel dual COX2 and sHE (soluble epoxide hydrolase) inhibitor. Treatment with PTUPB reduced body weight, liver weight, liver triglyceride and cholesterol content, and the expression of lipolytic/lipogenic and lipid uptake related genes (Acc, Cd36, and Cidec) in HFD mice. This made it be a promising potential therapy for liver steatosis associated with obesity.

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

货号:A1258087 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 COX COX-1 COX-2 其他靶点 纯度
Piroxicam {[allProObj[0].p_purity_real_show]}
Salicylic acid {[allProObj[0].p_purity_real_show]}
Phenacetin {[allProObj[0].p_purity_real_show]}
Etodolac {[allProObj[0].p_purity_real_show]}
Flunixin meglumine {[allProObj[0].p_purity_real_show]}
Ibuprofen L-lysine {[allProObj[0].p_purity_real_show]}
Nabumetone {[allProObj[0].p_purity_real_show]}
Acemetacin {[allProObj[0].p_purity_real_show]}
Diflunisal {[allProObj[0].p_purity_real_show]}
Pranoprofen {[allProObj[0].p_purity_real_show]}
Ampiroxicam {[allProObj[0].p_purity_real_show]}
Meloxicam {[allProObj[0].p_purity_real_show]}
Sulindac {[allProObj[0].p_purity_real_show]}
Ketoprofen {[allProObj[0].p_purity_real_show]}
Mefenamic Acid {[allProObj[0].p_purity_real_show]}
Bromfenac sodium {[allProObj[0].p_purity_real_show]}
Oxaprozin {[allProObj[0].p_purity_real_show]}
Aspirin {[allProObj[0].p_purity_real_show]}
Nepafenac {[allProObj[0].p_purity_real_show]}
Zaltoprofen {[allProObj[0].p_purity_real_show]}
Salicin {[allProObj[0].p_purity_real_show]}
Suprofen {[allProObj[0].p_purity_real_show]}
Xanthohumol {[allProObj[0].p_purity_real_show]}
Parecoxib {[allProObj[0].p_purity_real_show]}
Tolfenamic Acid +++

COX-2, IC50: 0.2 μM

{[allProObj[0].p_purity_real_show]}
Etoricoxib {[allProObj[0].p_purity_real_show]}
Niflumic Acid {[allProObj[0].p_purity_real_show]}
Valdecoxib ++++

COX-2, IC50: 5 nM

{[allProObj[0].p_purity_real_show]}
Ibuprofen +

COX-1, IC50: 13 μM

+

COX-2, IC50: 370 μM

{[allProObj[0].p_purity_real_show]}
Indomethacin ++

COX1, IC50: 0.28 μM

+

COX-2, IC50: 14 μM

{[allProObj[0].p_purity_real_show]}
Lornoxicam ++++

COX-1, IC50: 5 nM

++++

COX-2, IC50: 8 nM

{[allProObj[0].p_purity_real_show]}
Meclofenamic acid sodium ++++

COX-1, IC50: 40 nM

+++

COX-2, IC50: 50 nM

{[allProObj[0].p_purity_real_show]}
Rofecoxib ++++

COX-2, IC50: 18 nM

{[allProObj[0].p_purity_real_show]}
Asaraldehyde {[allProObj[0].p_purity_real_show]}
Naproxen +

COX-1, IC50: 8.7 μM

+

COX-2, IC50: 5.2 μM

{[allProObj[0].p_purity_real_show]}
Diclofenac Sodium Salt +++

COX-1, IC50: 60 nM

+++

COX-2, IC50: 200 nM

{[allProObj[0].p_purity_real_show]}
NS-398 ++

COX-2, IC50: 3.8 μM

{[allProObj[0].p_purity_real_show]}
Amfenac Sodium Hydrate ++

COX-1, IC50: 250 nM

+++

COX-2, IC50: 150 nM

{[allProObj[0].p_purity_real_show]}
Nimesulide +

COX-2, IC50: 26 μM

{[allProObj[0].p_purity_real_show]}
Lumiracoxib ++

COX-1, Ki: 3 μM

+++

COX-2, Ki: 60 nM

{[allProObj[0].p_purity_real_show]}
Rutaecarpine {[allProObj[0].p_purity_real_show]}
Celecoxib ++++

COX-2, IC50: 40 nM

{[allProObj[0].p_purity_real_show]}
Carprofen ++++

canine COX2, IC50: 30 nM

{[allProObj[0].p_purity_real_show]}
Ketorolac ++

COX-1 (human), IC50: 1.23 μM

++

COX-2 (human), IC50: 3.50 μM

{[allProObj[0].p_purity_real_show]}
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

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

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

动物实验配方
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