2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. PPAR Phosphatase
  4. PPARα agonist 5

PPARα agonist 5 是一种口服有效选择性 PPARα 部分激动剂 (EC50: 3 nM)。 PPARα agonist 5 减少脂质积累并上调 PPARα 靶基因，发挥抗脂肪肝作用。PPARα agonist 5 还通过部分 PPARγ 激动活性和对蛋白酪氨酸磷酸酶 1B (PTP1B) 的轻度抑制 (IC50: 79.1 μM)，表现出显著的降血脂和降血糖作用。PPARα agonist 5 具有良好的安全性，可用于血脂异常的 2 型糖尿病的研究。

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PPARα agonist 5 Chemical Structure

PPARα agonist 5 Chemical Structure

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PPARα agonist 5 相关抗体

Top Publications Citing Use of Products

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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 agonist 5 is an orally available, selective partial agonist of PPARα (EC50: 3 nM). PPARα agonist 5 reduces lipid accumulation and upregulates key PPARα target genes, exerting anti-fatty liver effects. PPARα agonist 5 also exhibits significant hypolipidemic and hypoglycemic effects through partial PPARγ agonist activity and mild inhibition of protein tyrosine phosphatase 1B (PTP1B) (IC50: 79.1 μM). PPARα agonist 5 has a good safety profile and can be used in the study of type 2 diabetes with dyslipidemia[1].

IC50 & Target

PPARα

3 nM (EC50)

PPAR-γ

1.66 μM (EC50)

PPARδ

>25 μM (EC50)

体外研究
(In Vitro)

PPARα agonist 5 (Compound (S)-2) 在 HepG2 细胞中选择性激动 PPARα (EC50: 3 nM)，对 PPARα 的活性比对 PPARγ (EC50: 1.66 μM) 高约 550 倍，且对 PPARδ 无显著活性[1]。
PPARα agonist 5 (0.025-25 μM, 24 h/15days) 在 HepaRG 细胞中显著减少由油酸诱导的脂质积累，并且上调了与脂肪酸氧化相关的 PPARα 靶基因，表明其通过激活脂质代谢通路发挥抗脂肪肝作用[1]。

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

PPARα agonist 5 相关抗体:

Real Time qPCR[1]

Cell Line: oleic acid (500 μM) treated HepaRG cells
Concentration: 0.025, 0.25, 2.5, 25 μM
Incubation Time: oleic acid for 24 hours, then for another 24 hours or 15 days
Result: Significantly upregulated fatty acid oxidation-related genes (CPT1a, HMGCS2, PDK4), and the activation of these genes indicated that it promoted fatty acid oxidation and reduced liver fat accumulation.
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Mice 1 mg/kg i.v. Cmin 11700 ng/mL
Mice 5 mg/kg p.o. Cmax 5880 ng/mL
Mice 1 mg/kg i.v. AUC0-t 8160 ng·h/mL
Mice 5 mg/kg p.o. Tmax 1 hr
Mice 1 mg/kg i.v. AUC0-inf 8620 ng·h/mL
Mice 5 mg/kg p.o. AUC0-t 35700 ng·h/mL
Mice 1 mg/kg i.v. T1/2 3.21 hr
Mice 5 mg/kg p.o. AUC0-inf 37200 ng·h/mL
Mice 1 mg/kg i.v. Vd 0.536 L/kg
Mice 5 mg/kg p.o. T1/2 5.63 hr
Mice 1 mg/kg i.v. CL 1.99 mL/min/kg
Mice 5 mg/kg p.o. Vd 1.12 L/kg
Mice 1 mg/kg i.v. MRT0-t 2.32 hr
Mice 5 mg/kg p.o. CL 2.27 mL/min/kg
Mice 5 mg/kg p.o. MRT0-t 5.58 hr
Mice 5 mg/kg p.o. F 87.6 %
体内研究
(In Vivo)

PPARα agonist 5 (Compound (S)-2) (1-7.5 mg/kg, p.o. 7 consecutive days) 在 Tyloxapol (HY-B1068) 诱导的高血脂糖尿病小鼠模型中表现出显著的降血脂和降血糖作用，并且对动脉、肾脏、肝脏和胰腺无毒性，并能改善高血脂引起的组织损伤[1]。

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

Animal Model: Swiss Albino mice (male, weight 25-30 g) injected with Tyloxapol (400 mg/kg)[1]
Dosage: (1, 3, 7.5 mg/kg)
Administration: p.o. 7 consecutive days
Result: Significantly reduced total cholesterol (TC), triglycerides (TG), low-density lipoprotein (LDL-C) and very low-density lipoprotein (VLDL-C) levels.
Showed significant hypoglycemic effects, which were associated with its partial PPARγ agonist activity and mild inhibition of protein tyrosine phosphatase 1B (PTP1B).
Was non-toxic to arteries, kidneys, liver and pancreas at a dose of 3 mg/kg, and was able to reverse organ damage caused by hyperlipidemia.
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 agonist 5 相关分类

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  • 稀释计算器

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质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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 agonist 5PPARα agonist5PPARα agonist-5PPARPhosphatasePeroxisome proliferator-activated receptorshypolipidemic and hypoglycemic activityHepaRG cellsHyperlipidemic micePTP1BInhibitorinhibitorinhibit

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