2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Cell Cycle/DNA Damage
  3. FABP PPAR
  4. ABP/PPAR modulator 1

ABP/PPAR modulator 1 是一种具有口服活性的 FABP 和 PPAR 多重调节剂 (FABP1 和 FABP4 的 IC50 分别为 0.65 μM 和 1.08 μM，PPARα、PPARγ 和 PPARδ 的 EC50 分别为 9.19 μM、2.20 μM 和 1.58 μM)。ABP/PPAR modulator 1 具有强效的抗代谢功能障碍相关脂肪性肝炎 (MASH) 活性。ABP/PPAR modulator 1 剂量依赖性地改善 WD + Carbon tetrachloride 诱导的 MASH 小鼠模型脂肪肝的多种病理特征。

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ABP/PPAR modulator 1 Chemical Structure

ABP/PPAR modulator 1 Chemical Structure

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ABP/PPAR modulator 1 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

ABP/PPAR modulator 1 is an orally active FABP and PPAR multiple modulator (IC50s of 0.65  μM and 1.08  μM for FABP1 and FABP4, EC50 s of 9.19  μM, 2.20  μM and 1.58 μM for PPARα, PPARγ and PPARδ). ABP/PPAR modulator 1 has potent anti-metabolic dysfunction-associated steatohepatitis (MASH) activity. ABP/PPAR modulator 1 dose-dependently ameliorates multiple pathological characteristics of fatty liver in WD + Carbon tetrachloride-induced MASH mice model[1].

IC50 & Target[1]

PPARα

9.19 μM (EC50)

PPARγ

2.20 μM (EC50)

PPARδ

1.58 μM (EC50)

FABP1

0.65 μM (IC50)

FABP4

1.08 μM (IC50)

体外研究
(In Vitro)

ABP/PPAR modulator 1 (Compound 27) 对 PPAR 具有优异的结合能力 (PPARα、 PPARγ 和 PPARδ 的 Kd 分别为 5.23 μM、 0.98 μM 和 0.76 μM)[1]。
ABP/PPAR modulator 1 (10 mM-0.1 μM) 对 FABP1 的亲和力高于其内源性配体亚油酸 (LA) (Kd: 5.885 μM vs. LA: 14.281 μM)[1]。

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

ABP/PPAR modulator 1 相关抗体:
体内研究
(In Vivo)

ABP/PPAR modulator 1 (Compound 27) (5-20 mg/kg，口服，每日一次，持续 4 周) 剂量依赖性地降低西方饮食联合低剂量Carbon tetrachloride (HY-Y0298) (CCl4) (WD + Carbon tetrachloride) 诱导的 MASH 小鼠的肝重量、肝重与体重的比率和 NAS 评分，同时抑制炎症、减弱纤维化并缓解的氧化应激，且在较高剂量下抗 MASH 疗效增强[1]。
ABP/PPAR modulator 1 (20 mg/kg，口服，每日一次，持续 4 周) 显著降低 MASH 小鼠模型中 TC 和肝脏 TG 水平[1]。
ABP/PPAR modulator 1 (10 mg/kg，口服，每日一次，持续 4 周) 显著降低MASH 小鼠模型中肝脏 LDH、血清 AST、 ALT、 TBA 和 TBIL 水平，且不影响 ALP 水平[1]。

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

Animal Model: male C57BL/6 mice (6 weeks old) were given a high-sugar diet (18.9 g/L glucose and 23.1 g/L fructose) and a high-fat feed (41 % sucrose, 21.1 % fat, and 1.25 % cholesterol) with 2 % CCl4 olive oil (i.p., once a week for 12 weeks) to induce MASH
Dosage: 5, 10, 20 mg/kg
Administration: p.o., once a day for 4 weeks, and then collects liver tissues.
Result: Dose-dependently reduced the liver weight, the liver weight to body weight ratio and NAS scores of MASH mice, with its anti-MASH efficacy significantly improving as the dosage increased.
Dose-dependently decreased MPO expression levels and downregulated MCP-1, TNF-α, IL-1β, and IL-6 mRNA expression in MASH mice model.
Significantly reduced the levels of liver of TC, hepatic TG levels liver LDH, serum AST, ALT, TBA, and TBIL, and did not affect the ALP level in MASH mice model.
Increased the levels of SOD, GSH-Px, and GST, and decreased MDA content, protecting the liver from oxidative stress in MASH mice model.
Significantly reduced the expression ofα-SMA, TGF-β and HYP levels, inhibiting the activation of hepatic stellate cells and the liver fibrosis in MASH mice model.
分子量

561.67

Formula

C33H39NO7
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

ABP/PPAR modulator 1 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:

ABP/PPAR modulator 1FABPPPARFatty acid-binding proteinPeroxisome proliferator-activated receptorsMetabolic dysfunction-associated steatohepatitis (MASH)FABPsPPARsLipid metabolismOxidative stressFibrosisInflammationInhibitorinhibitorinhibit

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