PTUPB is a potent and dual sEH and COX-2 enzymes inhibitor with IC₅₀ of 0.9 nM and 1.26 μM, respectively^[1].

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

543.56

C₂₆H₂₄F₃N₅O₃S

1287761-01-6

Room temperature in continental US; may vary elsewhere.

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

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。

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。

• [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.

  [3]. Hwang SH, 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.