2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. PPAR
  4. PPARδ agonist 13

PPARδ agonist 13 是一种强效、选择性且口服活性的 PPARδ 激动剂，其 EC50 值为 0.50 nM。PPARδ agonist 13 可结合至 PPARδ 配体结合口袋，并上调 PPARδ 靶基因的表达。PPARδ agonist 13 可抑制肾成纤维细胞活化、恢复脂肪酸氧化，并减弱 TGF-β1 诱导的肾成纤维细胞活化。PPARδ agonist 13 在单侧输尿管梗阻小鼠模型中展现出抗肾纤维化作用。PPARδ agonist 13 可用于肾纤维化的相关研究。

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PPARδ agonist 13

PPARδ agonist 13 Chemical Structure

CAS No. : 3056618-93-7

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PPARδ agonist 13 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 13 is a potent, selective and orally active PPARδ agonist with an EC50 values of 0.50 nM. PPARδ agonist 13 binds to the PPARδ ligand-binding pocket and upregulates PPARδ target gene expression. PPARδ agonist 13 inhibits renal fibroblast activation, restores fatty acid oxidation, and attenuates TGF-β1-induced renal fibroblast activation. PPARδ agonist 13 exhibits anti-renal fibrosis effects in a mouse model of unilateral ureteral obstruction. PPARδ agonist 13 can be used for the research of renal fibrosis[1].

IC50 & Target[1]

PPARδ

0.5 nM (EC50)

PPARα

>10000 nM (EC50)

PPARγ

>10000 nM (EC50)

体外研究
(In Vitro)

PPARδ agonist 13 (Compound 16a) (10-1000 nM; 6 h) 可在 HK2 细胞中呈剂量依赖性上调 PPARδ 靶基因的表达[1]。
PPARδ agonist 13 (0.2-5 μM; 16 h) 在 Cos-7 细胞中对 PPARδ 表现出高选择性，仅在最高测试浓度 5 μM 下观察到微弱的 PPARγ 激动活性[1]。
PPARδ agonist 13 (1-30 μM; 3 min) 可直接与纯化的 PPARδ LBD 蛋白相互作用，这一点可通过降低 ANS 荧光的结果得到证明[1]。
PPARδ agonist 13 (0.3-30 μM) 在 hERG 敲入型 HEK293 细胞中不会抑制 hERG 钾离子通道，提示其心血管风险较低[1]。
PPARδ agonist 13 (2.5-10 nM; 23 h) 可剂量依赖性地减弱 TGF-β1 诱导的 NRK-49F 肾成纤维细胞活化，在 2.5 和 10 nM 浓度下降低 α-SMA 和纤连蛋白的表达[1]。

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

PPARδ agonist 13 相关抗体:

RT-PCR[1]

Cell Line: Human renal proximal tubule HK2 cells
Concentration: 10, 100, 1000 nM
Incubation Time: 6 h
Result: Dose-dependently upregulated the expression of PPARδ target genes ANGPTL4, PDK4, and CPT1A in HK2 cells.

Western Blot Analysis[1]

Cell Line: NRK-49F cells
Concentration: 2.5, 10 nM
Incubation Time: 23 h (after 1 h TGF-β1 pre-treatment)
Result: Dose-dependently suppressed the TGF-β1-induced expression of fibrotic markers α-SMA and fibronectin in NRK-49F cells.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Cmax AUC0-∞ CL F
Rat[1] 2 mg/kg i.v. 2.59 ± 0.79 h 44697 ± 13239 ng/mL 31986 ± 2943 ng·h/mL 0.06 ± 0.01 L/h/kg /
Rat[1] 10 mg/kg p.o. 2.60 ± 0.45 h 16133 ± 4332 ng/mL 69196 ± 14574 ng·h/mL 0.15 ± 0.04 L/h/kg 43 %
体内研究
(In Vivo)

PPARδ agonist 13 (3-10 mg/kg；灌胃；每日；13 天) 可通过下调纤维化基因表达、减轻炎症反应、抑制细胞凋亡及恢复脂肪酸氧化通路，以剂量依赖方式改善雄性 C57BL/6JNifdc 小鼠中单侧输尿管梗阻诱导的肾纤维化[1]。
PPARδ agonist 13 (以 100 mg/kg 剂量连续给药 14 天，或以 2000 mg/kg 单次给药；灌胃）在 C57BL/6JNifdc 小鼠体内表现出低毒性[1]。

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

Animal Model: C57BL/6JNifdc (male, 7-8 weeks old, ~22 g, nilateral ureteral obstructio model)[1]
Dosage: 3 mg/kg; 10 mg/kg
Administration: I.g.; daily; 13 days
Result: Relieved UUO-induced tubular atrophy and dilation.
Significantly reduced UUO-induced collagen accumulation and decreased protein expression of collagen I and collagen III.
Potently downregulated UUO-induced upregulation of α-SMA protein levels and mRNA expression of fibrotic genes (Acta2, Col1a1, Col3a1, Col4a1, Fn1, Vim, Tgfb1, Ctgf).
Reduced UUO-induced renal interstitial inflammatory cell infiltration and dose-dependently suppressed elevated mRNA levels of pro-inflammatory cytokines/chemokines (Tnf, Il1b, Il6, Ccl4, Ccl5).
Decreased protein levels of phosphorylated NF-κB p65 and phosphorylated JNK, and increased the antiapoptotic Bcl-2 to pro-apoptotic Bax protein ratio to mitigate UUO-induced renal apoptosis.
Dose-dependently restored UUO-downregulated mRNA expression of fatty acid oxidation-related genes (Cpt1a, Cpt2, Acadm, Acadvl, Acads, Ppargc1a) in kidney tissue.
分子量

520.48

Formula

C27H24F3N2NaO4
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 13 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

PPARδ agonist 133056618-93-7PPARδ agonist13PPARδ agonist-13PPARPeroxisome proliferator-activated receptorsPPARδCos-7 cellsNRK-49F renal fibroblastsrenal fibroblastrenal fibrosismouse model of unilateral ureteral obstructionHK2 cellshERG knock-in HEK293 cellsPPARδ ligand-binding pocketTGF-β1Inhibitorinhibitorinhibit

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