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

PPAR agonist 4 (Compound 12) 是一种口服有效的 PPAR 激动剂，可激活 PPARα，PPARδ 和 PPARγ，EC50分别为 0.7，0.7 和 1.8 μM。PPAR agonist 4 具有抗肝纤维化活性。

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PPAR agonist 4 Chemical Structure

PPAR agonist 4 Chemical Structure

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PPAR 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

PPAR agonist 4 (Compound 12) is an orally active agonist for peroxisome proliferator-activated receptor (PPAR), which activates PPARα, PPARδ and PPARγ with EC50s of 0.7, 0.7 and 1.8 μM, respectively. PPAR agonist 4 exhibits anti-liver fibrosis efficacy[1].

IC50 & Target

PPARα

0.7 μM (EC50)

PPARδ

0.7 μM (EC50)

PPARγ

1.8 μM (EC50)

体外研究
(In Vitro)

PPAR agonist 4 (3-10 μM) 剂量依赖性地上调 HepG2 细胞中 PPARα/δ 靶基因 CPT1A，PDK4 和 ANGPTL4 以及 HEK293 细胞中 PPARγ 靶基因 CD36 和 FABP4 的表达[1]。

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

PPAR agonist 4 相关抗体:

RT-PCR[1]

Cell Line: HepG2 and HEK293
Concentration: 3-10 μM
Incubation Time: 12 h
Result: Upregulated levels of CPT1A, PDK4 and ANGPTL4, downregulated levels of CD36 and FABP4.
体内研究
(In Vivo)

PPAR agonist 4 (3-30 mg/kg，口服，3 周) 可改善 CCl4 诱导的肝纤维化小鼠模型中的胶原沉积并抑制炎症细胞浸润[1]。

PPAR agonist 4 在SD 大鼠体内的药代动力学分析[1]

route Dose (mg/kg) T1/2 (h) MRT (h) Cmax (μM) AUC0-t (h·μM) F (%)
i.v. 2 9.7 6.8 12.2 59.8 -
p.o. 10 17.0 10.1 15.9 274.5 91.8

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

Animal Model: CCL4-induced liver fibrosis in C57BL/6 mice[1]
Dosage: 3-30 mg/kg
Administration: p.o., once a day for 3 weeks
Result: Reduced levels of collagen and α-SMA, reduced accumulation of collagen and inflammatory cell infiltration in the portal area.
Upregulated the expression of PPARs target genes (Cpt1a, Cpt2, Angptl4 and Cd36).
分子量

451.48

Formula

C23H28F3N3O3
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 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:

PPAR agonist 4PPAR agonist4PPAR agonist-4PPARPeroxisome proliferator-activated receptorsliver fibrosisSprague-Dawley ratsInhibitorinhibitorinhibit

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PPAR agonist 4
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HY-163443
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