GlpBio

PTUPB

目录号: GC60311纯度: >98.00%
PTUPB是一种新型的COX-2和sEH双抑制剂，IC50 值分别为 1.26 nM 和 0.9μM。
PTUPB
Cas No.: 1287761-01-6
规格价格库存数量操作
1mg¥267.00现货
1
5mg¥700.00现货
1
10mg¥1,180.00现货
1
25mg¥2,200.00现货
1
10mM (in 1mL DMSO)¥837.00现货
1
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产品描述 Description

PTUPB is a novel dual COX-2 and sEH inhibitor with IC50 values of 1.26 nM and 0.9 μM, respectively[1]. It has certain anti-tumor and anti-inflammatory effects[2].

PTUPB(10, 100, 1000, and 10000 nM;1h) inhibits the activation of NLRP3 inflammasome in primary murine macrophages by reduced the protein expression of caspase-1 p10 and IL-1β p17 in macrophages [3]. PTUPB (10, 20, 25 or 30 μM; 72 h) inhibits glioblastoma cell proliferation and G1 phase cell cycle arrest in vitro, and suppresses the tumor growth and angiogenesis in vivo[4].

PTUPB(5 mg/kg; 1 h before the LPS administration; s.c) decreased the pro-inflammatory factors, oxidative stress, and activation of NACHT, LRR, and PYD domains-containing protein 3 (NLRP3) inflammasome in LPS-induced ALI mice [3]. PTUPB(10 mg/kg/d; 8 weeks) attenuates renal inflammation and oxidative stress in Zucker diabetic fatty(ZDF) rats[5]. PTUPB(5 mg/kg; s.c) treatment suppressed the activation of NLRP3 inflammasome in the liver and lung of septic mice[6]. PTUPB (5 mg/kg; s.c; once a day for 14days) alleviated the pathological changes in lung tissue and collagen deposition, as well as reduced senescence marker molecules (p16Ink4a and p53-p21Waf1/Cip1) in the lungs of mice treated by bleomycin (BLM) [7].

References:
[1]. Hwang SH, Wagner KM, et,al. Synthesis and structure-activity relationship studies of urea-containing pyrazoles as dual inhibitors of cyclooxygenase-2 and soluble epoxide hydrolase. J Med Chem. 2011 Apr 28;54(8):3037-50. doi: 10.1021/jm2001376. Epub 2011 Apr 5. PMID: 21434686; PMCID: PMC3281519.
[2]. Wang F, Zhang H, et,al. COX-2/sEH Dual Inhibitor PTUPB Potentiates the Antitumor Efficacy of Cisplatin. Mol Cancer Ther. 2018 Feb;17(2):474-483. doi: 10.1158/1535-7163.MCT-16-0818. Epub 2017 Dec 28. PMID: 29284644; PMCID: PMC5824635.
[3]. Yang HH, Duan JX, et,al. A COX-2/sEH dual inhibitor PTUPB alleviates lipopolysaccharide-induced acute lung injury in mice by inhibiting NLRP3 inflammasome activation. Theranostics. 2020 Mar 26;10(11):4749-4761. doi: 10.7150/thno.43108. PMID: 32308747; PMCID: PMC7163435.
[4]. Li J, Zhou Y, et,al. COX-2/sEH dual inhibitor PTUPB suppresses glioblastoma growth by targeting epidermal growth factor receptor and hyaluronan mediated motility receptor. Oncotarget. 2017 Sep 15;8(50):87353-87363. doi: 10.18632/oncotarget.20928. PMID: 29152086; PMCID: PMC5675638.
[5]. Hye Khan MA, Hwang SH, et,al. A dual COX-2/sEH inhibitor improves the metabolic profile and reduces kidney injury in Zucker diabetic fatty rat. Prostaglandins Other Lipid Mediat. 2016 Sep;125:40-7. doi: 10.1016/j.prostaglandins.2016.07.003. Epub 2016 Jul 16. PMID: 27432695; PMCID: PMC5035206.
[6]. Zhang YF, Sun CC, et,al. A COX-2/sEH dual inhibitor PTUPB ameliorates cecal ligation and puncture-induced sepsis in mice via anti-inflammation and anti-oxidative stress. Biomed Pharmacother. 2020 Jun;126:109907. doi: 10.1016/j.biopha.2020.109907. Epub 2020 Feb 27. PMID: 32114358; PMCID: PMC8868492.
[7]. Zhang CY, Duan JX, et,al. COX-2/sEH dual inhibitor PTUPB alleviates bleomycin-induced pulmonary fibrosis in mice via inhibiting senescence. FEBS J. 2020 Apr;287(8):1666-1680. doi: 10.1111/febs.15105. Epub 2019 Nov 8. PMID: 31646730; PMCID: PMC7174142.

PTUPB是一种新型的COX-2和sEH双抑制剂，IC50值分别为1.26 nM和0.9 μM[1]。具有一定的抗肿瘤、抗炎作用[2]。

PTUPB(10、100、1000和10000 nM;1h)通过降低巨噬细胞中caspase-1 p10和IL-1β p17的蛋白表达，抑制小鼠原代巨噬细胞NLRP3炎性体的激活[3]。PTUPB(10、20、25或30 μM;72 h)体外抑制胶质母细胞瘤细胞增殖和G1期细胞周期阻滞，体内抑制肿瘤生长和血管生成[4]。

PTUPB(5 mg/kg; 1 h before the LPS administration; s.c)可降低脂多糖诱导的ALI小鼠的促炎因子、氧化应激以及NACHT、LRR和 NLRP3的活化[3]。PTUPB(10 mg/kg/d; 8 weeks)可减轻Zucker糖尿病脂肪(ZDF)大鼠的肾脏炎症和氧化应激[5]。PTUPB(5 mg/kg; s.c)治疗可抑制脓毒症小鼠肝脏和肺部NLRP3炎性体的激活[6]。PTUPB(5 mg/kg; s.c; once a day for 14days)减轻了博来霉素(BLM)处理小鼠肺组织的病理改变和胶原沉积，降低了衰老标志物分子(p16Ink4a和p53-p21Waf1/Cip1)[7]。

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

 Primary murine peritoneal macrophages

Preparation Method

 Macrophages were treated with LPS (100 ng/mL) for 6 h with or without PTUPB pre-treatment (10, 100, and 1000 nM) for 1 h and activity of LDH in the supernatant was detected.

Reaction Conditions

 10, 100, 1000, and 10000 nM;1h

Applications

 PTUPB pretreatment at concentrations of 10, 100, and 1000 nM significantly decreased the LDH activity triggered by LPS.
Animal experiment [1]:

Animal models

 Acute lung injury (ALI) C57BL/6 mice

Preparation Method

 Mice were subcutaneously injected with PTUPB (5 mg/kg) dissolved in PEG400 1 h prior to ALI. Specifically, The mice were randomly assigned to four groups: control, PTUPB, ALI, and ALI + PTUPB. ALI was induced by administering an intratracheal injection of LPS (5 mg/kg) dissolved in 50 μL of sterile saline. Mice in the PTUPB and PTUPB + ALI groups received a subcutaneous injection of PTUPB (5 mg/kg) dissolved in PEG400, one hour before the intratracheal injection. For the control and ALI groups, PEG400 was administered subcutaneously.

Dosage form

 5 mg/kg; 1 h before the LPS administration (ALI); s.c

Applications

 PTUPB mitigates the pathological lung damage and restores the respiratory function in mice exposed to LPS.
Kinase experiment [1]:

Preparation Method

For the recombinant affinity purified sEHs (human, mouse, and rat), we used a fluorescent-based assay to determine IC50s.
Enzymes (∼1 nM human sEH) were incubated with PTUPB for 5 min in 25 mM Bis-Tris/HCl buffer (200 μL; pH 7.0) at 30 °C before substrate (cyano(2-methoxynaphthalen-6-yl)methyl trans-(3-phenyl-oxyran-2-yl)methyl carbonate (CMNPC) was added.
Activity was assessed by measuring the appearance of the fluorescent 6-methoxynaphthaldehyde product (λem= 330 nm, λex = 465 nm) at 30 ℃ during a 10 min incubation.

Applications

 PTUPB is sEH inhibitor with IC50 values of 0.9 μM.

References:
[1]. Yang HH, Duan JX, et,al. A COX-2/sEH dual inhibitor PTUPB alleviates lipopolysaccharide-induced acute lung injury in mice by inhibiting NLRP3 inflammasome activation. Theranostics. 2020 Mar 26;10(11):4749-4761. doi: 10.7150/thno.43108. PMID: 32308747; PMCID: PMC7163435.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
1287761-01-6
SMILES
O=S(C1=CC=C(N2N=C(CCCNC(NC3=CC=C(C(F)(F)F)C=C3)=O)C=C2C4=CC=CC=C4)C=C1)(N)=O
分子式
C26H24F3N5O3S
分子量
543.56 g/mol
溶解性
DMSO: 100 mg/mL (183.97 mM)
保存条件
Store at -20°C
General tips
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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol