2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease GPCR/G Protein
  3. PPAR Adenosine Receptor Fatty Acid Synthase (FASN) Endogenous Metabolite
  4. PPAR agonist 7

PPAR agonist 7 是一种具有口服活性的泛 PPAR 激动剂，能够有效激活所有三种亚型：PPARα (EC50 = 1.51 μM) 、PPARδ (EC50 = 1.11 μM) 和 PPARγ (EC50 = 3.14 μM)。PPAR agonist 7 显著增强脂肪细胞对葡萄糖的摄取，同时脂肪生成活性极低。PPAR agonist 7 能够抑制白色脂肪组织中 PPARγ Ser273 的磷酸化，并上调胰岛素增敏基因。在高脂饮食 (HFD)/ Streptozotocin (HY-13753) (STZ) 诱导的 2 型糖尿病 (T2DM) 模型中，PPAR agonist 7 不会引起体重增加或体液潴留。PPAR agonist 7 能够选择性地调节 PPAR 信号通路，而不会激活脂肪生成基因程序。PPAR agonist 7 可用于糖尿病的研究。

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PPAR agonist 7

PPAR agonist 7 Chemical Structure

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PPAR agonist 7 相关抗体

Top Publications Citing Use of Products

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PPARα PPARβ/δ PPARγ PPAR PPARδ

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Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PPAR agonist 7 is an orally active pan-PPAR agonist, demonstrating potent activation of all three subtypes, PPARα (EC50 = 1.51 μM), PPARδ (EC50 = 1.11 μM), and PPARγ (EC50 = 3.14 μM). PPAR agonist 7 significantly enhances glucose uptake in adipocytes while exhibiting minimal adipogenic activity. PPAR agonist 7 can suppress PPARγ Ser273 phosphorylation in white adipose tissue and upregulate insulin-sensitizing genes. PPAR agonist 7 does not cause weight gain or fluid retention in high-fat diet (HFD)/ Streptozotocin (HY-13753) (STZ)-induced type 2 diabetes mellitus (T2DM) models. PPAR agonist 7 has selective modulation of PPAR signaling pathways without activation of adipogenic gene programs. PPAR agonist 7 can be used for the study of diabetes[1].

体外研究
(In Vitro)

PPAR agonist 7 (Compound 1d) (1-10 μM，24 小时) 对 3T3-L1 脂肪细胞的活力无显著影响，但在测试浓度下，其能以剂量依赖的方式增加成熟脂肪细胞的葡萄糖摄取[1]。
PPAR agonist 7 (10 μM，75 分钟) 可显著抑制 3T3-L1 细胞中 TNFα 诱导的 PPARγ 在Ser273 位点的磷酸化[1]。
PPAR agonist 7 (1-10 μM，24 小时) 可显著恢复暴露于 30 mM 葡萄糖和 0.5 μM 胰岛素的 HepG2细胞的葡萄糖摄取[1]。
PPAR agonist 7 (10 μM，8 天) 可显著减少 3T3-L1 细胞中的脂滴数量，且脂肪生成关键基因 (Ppary、Ap2、Cebpa、Fasn、Cd36、Lpl) 的 mRNA 水平未见显著上调[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

PPAR agonist 7 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: 3T3-L1 adipocytes cells
Concentration: 1 μM, 5 μM, 10 μM
Incubation Time: 24 h
Result: Showed no significant effect on the viability of 3T3-L1 adipocytes.

Western Blot Analysis[1]

Cell Line: TNF-α-induced 3T3-L1 cells
Concentration: 10 μM
Incubation Time: Pretreated for 45 min, then stimulation with 50 ng/mL TNF-α for an additional 30 min
Result: Significantly inhibited TNFα-induced phosphorylation of PPARγ at Ser273 in 3T3-L1 cells.

Real Time qPCR[1]

Cell Line: 3T3-L1 adipocytes cells
Concentration: 10 μM
Incubation Time: 8 days
Result: Showed no significant effects on any of these adipogenesis-related genes (Ppary, Ap2, Cebpa, Fasn, Cd36, Lpl).
体内研究
(In Vivo)

PPAR agonist 7 (Compound 1d) (5-20 mg/kg，口服，每日一次，持续 30 天) 显著改善了小鼠 T2DM 模型中的胰岛素敏感性、血糖控制和脂质代谢，且不引起体重增加或体液潴留等副作用[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: The male C57BL/6J mice (18-22 g, 4-6 weeks) were fed a high-fat diet 12 weeks and then mice were received daily intraperitoneal injections of streptozotocin (STZ; 50 mg/kg) for five consecutive days, following this, the mice were fed for an additional three weeks to establish the STZ/HFD-induced T2DM model[1].
Dosage: 5 mg/kg, 10 mg/kg, 20 mg/kg
Administration: P.o., once daily for 30 days
Result: Significantly improved fasting blood glucose levels and reduced fasting insulin concentrations.
Demonstrated dose-dependent improvements in insulin resistance in this diabetic model.
Significantly elevated fasting plasma adiponectin levels in T2DM mice.
Did not cause significant body weight gain and no effect on hematocrit.
Significantly enhanced glucose clearance and insulin sensitivity.
Significantly reduced plasma TG, TC, LDL-C, and FFA; significantly increased plasma adiponectin levels.
Significantly alleviated hepatocellular steatosis and ballooning degeneration; reduced plasma AST and ALT levels.
Inhibited PPARγ Ser273 phosphorylation in WAT; upregulated insulin-sensitive genes (Adiponectin, Cyp2f2).
Selectively regulated insulin resistance-related genes (Glut4, Irs1), but did not activate adipogenesis genes (Ppary, Fasn).
分子量

477.59

Formula

C29H35NO5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PPAR agonist 7 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

PPAR agonist 7PPAR agonist7PPAR agonist-7PPARAdenosine ReceptorFatty Acid Synthase (FASN)Endogenous MetabolitePeroxisome proliferator-activated receptorsP1 receptorInsulin resistanceLipid metabolismPPAR modulatorsSer273 phosphorylationT2DMInhibitorinhibitorinhibit

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