2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. PPAR
  4. PPARα/γ agonist 4

PPARα/γ agonist 4 (Compound (S)-7) 是具口服有效性的 PPARα 和 PPARγ 的双重强效激活剂，EC50 值分别为 0.061 μM 和 1.42 μM。PPARα/γ agonist 4 通过胰岛素非依赖性机制起作用，具有线粒体丙酮酸载体抑制和抗糖尿病特性。PPARα/γ agonist 4 有望用于血脂异常型 2 型糖尿病领域研究。

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PPARα/γ agonist 4 Chemical Structure

PPARα/γ agonist 4 Chemical Structure

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PPARα/γ agonist 4 相关抗体

Top Publications Citing Use of Products

查看 PPAR 亚型特异性产品:

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PPARα PPARβ/δ PPARγ PPAR PPARδ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PPARα/γ agonist 4 (Compound (S)-7) is an orally active dual potent agonist of PPARα and PPARγ, with EC50 values of 0.061 μM and 1.42 μM respectively. PPARα/γ agonist 4 acts through an insulin-independent mechanism and exhibits mitochondrial pyruvate carrier inhibition and anti-diabetic properties. PPARα/γ agonist 4 is expected to be used in research for dyslipidemic type 2 diabetes[1].

IC50 & Target[1]

PPARα

 

PPAR-γ

 

体外研究
(In Vitro)

PPARα/γ agonist 4 (100 nM, 24 小时) 能够增加 C2C12 细胞系的葡萄糖的摄取和代谢，并通过增强脂肪酸降解的线粒体活性避免肝细胞或肌肉细胞中的脂质积累[1]。

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

PPARα/γ agonist 4 相关抗体:
体内研究
(In Vivo)

PPARα/γ agonist 4 (25 mg/kg, 50 mg/kg, 口服, 治疗15天) 在糖尿病小鼠模型中以剂量依赖方式发挥抗高血糖作用，同时具有显著降脂功效[1]。

药代动力学分析[1]

PPARα/γ agonist 4 Does Volume (mL/kg) C0/Cmax(ng/mL) Tmax (h) AUClast(h·ng/mL) AUCinfinity (h⋅ng/mL) T1/2 (h) Vd (L/kg) CL (mL/min/kg) MRTlast(h) F (%)
i.v. (1 mg/kg) 10 2300 0.083 11400 11800 4.74 0.581 1.42 6.04 -
p.o. (5 mg/kg) 10 4280 2 43600 49000 7.61 1.16 1.74 7.74 76.4

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

Animal Model: Streptozotocin (HY-13753) -induced diabetic mouse model[1]
Dosage: 25 mg/kg, 50 mg/kg
Administration: Oral gavage (p.o.), 15 days
Result: At a dose of 50 mg/kg exhibited greater hypoglycemic effects compared to the 25 mg/kg dose.
Oral treatment with PPARα/γ agonist 4 at 25 mg/kg significantly reduced levels of total cholesterol, high-density lipoprotein cholesterol (HDL-C), low-density lipoprotein cholesterol (LDL-C), and triglycerides.
The 50 mg/kg dose reduced total cholesterol and HDL-C levels, but showed a smaller improvement in triglyceride levels.
分子量

368.42

Formula

C25H20O3
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

PPARα/γ agonist 4 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PPARα/γ agonist 4PPARPeroxisome proliferator-activated receptorsC2C12 cell lineDiabetic mouse modelMitochondrial pyruvate carrier inhibitionAntidiabetic propertiesDiabetesInhibitorinhibitorinhibit

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