2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. PPAR
  4. PPARδ agonist 10

PPARδ agonist 10 (compound 7) 是一种具有口服活性、选择性的 PPARδ 部分激动剂，对 hPPARδ(LBD)-GAL4 和 mPPARδ 的 EC50 值分别为 0.053 μM 和 0.30 µM。PPARδ agonist 10 在反式激活测定中是部分 PPARδ 激动剂，但在体外和体内都是肌肉细胞游离脂肪酸氧化的完全激动剂。PPARδ agonist 10 可用于血脂异常研究。

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PPARδ agonist 10 Chemical Structure

PPARδ agonist 10 Chemical Structure

CAS No. : 685139-10-0

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PPARδ agonist 10 相关抗体

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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

PPARδ agonist 10 (compound 7) is an orally active, selective, and partial agonist of PPARδ, with EC50 values of 0.053 μM and 0.30 µM for hPPARδ(LBD)-GAL4 and mPPARδ, respectively. PPARδ agonist 10 is a partial PPARδ agonist in transactivation assay but a full agonist on free fatty acids (FFA) oxidation in muscle cells both in vitro and in vivo. PPARδ agonist 10 can be used for dyslipidemia research[1].

IC50 & Target

PPARδ

0.053 μM (EC50, hPPARδ)

PPARδ

0.30 μM (EC50, mPPARδ)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 EC50
> 10 μM
Compound: 7
Activity at human liver PPAR alpha expressed in HEK293 cells by PPAR-GAL4 transactivation assay
Activity at human liver PPAR alpha expressed in HEK293 cells by PPAR-GAL4 transactivation assay
[PMID: 17343371]
HEK293 EC50
> 10 μM
Compound: 7
Activity at human adipose tissue PPAR gamma expressed in HEK293 cells by PPAR-GAL4 transactivation assay
Activity at human adipose tissue PPAR gamma expressed in HEK293 cells by PPAR-GAL4 transactivation assay
[PMID: 17343371]
HEK293 EC50
0.053 μM
Compound: 7
Activity at human placenta PPAR delta expressed in HEK293 cells by PPAR-GAL4 transactivation assay
Activity at human placenta PPAR delta expressed in HEK293 cells by PPAR-GAL4 transactivation assay
[PMID: 17343371]
HEK293 EC50
0.3 μM
Compound: 7
Agonist activity at mouse PPAR delta expressed in HEK293 cells by PPAR-GAL4 transactivation assay
Agonist activity at mouse PPAR delta expressed in HEK293 cells by PPAR-GAL4 transactivation assay
[PMID: 17343371]
体外研究
(In Vitro)

PPARδ agonist 10 (compound 7) 可增加大鼠 L6 肌细胞中的脂肪酸氧化，EC50 为 30 nM[1]。

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

PPARδ agonist 10 相关抗体:
体内研究
(In Vivo)

PPARδ agonist 10 (compound 7) 以剂量依赖性方式改变血浆脂质参数，以减少动脉粥样硬化[1]。
PPARδ agonist 10 （5-20 mg/kg，口服，每日一次）在大鼠体内表现出良好的口服药代动力学特性[1]。

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

Animal Model: ApoB100/CETP-Tgn mice (female, 9-11 weeks old, with a mean body weight of 19.2 g±1.4, n=8/group, were fed a high fat diet)[1]
Dosage: 5, 10, and 20 mg/kg
Administration: PO, once daily, for 6 weeks
Result: Changed plasma lipid parameters in a dose-dependent manner to a less atherogenic profile, with increased HDL and decreased LDL and TG. HbA1c levels were lowered.
Animal Model: Male SD rats[1]
Dosage: 1.06 mg/kg (IV)/2.06 mg/kg (PO)
Administration: p.o. and i.v., single (Pharmacokinetic Analysis)
Result: Pharmacokinetic Parameters of PPARδ agonist 10 in male Sprague-Dawley rats[1].
IV (1.06 mg/kg) PO (2.06 mg/kg)
Cmax (ng/mL) 508
AUC0-24 (ng/mL∗min) 79294
t1/2 (min) 59
CL (mL/min/kg) 11.9
Vd, ss (L/kg) 0.3
F (%) 46%
分子量

568.71

Formula

C23H17Br2ClO3S
CAS 号
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

PPARδ agonist 10 相关分类

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  • 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:

PPARδ agonist 10685139-10-0PPARδ agonist10PPARδ agonist-10PPARPeroxisome proliferator-activated receptorsrat muscle L6 cellatherogenicdyslipidemiaInhibitorinhibitorinhibit

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