1. Metabolic Enzyme/Protease
  2. HIF/HIF Prolyl-Hydroxylase
  3. ZG-2291

ZG-2291 是一种靶向 FIH (缺氧诱导因子抑制剂) 的选择性抑制剂,具有口服活性。ZG-2291 通过与 FIH 结合,促使一个催化关键的酪氨酸发生构象翻转,从而实现对 FIH 的选择性抑制,而不会影响其他 JmjC 亚家族的 2OG 氧化酶。ZG-2291k 促进 ob/ob 小鼠的产热和改善肥胖症状和代谢功能障碍。ZG-2291 有望用于肥胖疾病领域的研究。

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ZG-2291 Chemical Structure

ZG-2291 Chemical Structure

CAS No. : 2962103-40-6

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查看 HIF/HIF Prolyl-Hydroxylase 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ZG-2291 is a selective inhibitor targeting FIH (Factor Inhibiting HIF) with oral activity. By binding to FIH, ZG-2291 promotes a conformational flip of a catalytically important tyrosine, enabling selective inhibition of FIH without affecting other 2OG oxygenases in the JmjC subfamily. ZG-2291k enhances thermogenesis in ob/ob mice and improves obesity-related symptoms and metabolic dysfunctions. ZG-2291 holds promise for research in the field of obesity-related diseases[1].

体外研究
(In Vitro)

ZG-2291 (5 或 20 μM,48 小时) 在 Hep3B 细胞中是一种具有活性的细胞穿透性 FIH 抑制剂[1]
ZG-2291 (5 或 20 μM,48 小时) 促进了 3T3-L1 衍生脂肪细胞中的产热作用并改善了脂质堆积[1]

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

Real Time qPCR[1]

Cell Line: Hep3B cells
Concentration: 5, 20 μM
Incubation Time: 48 h
Result: Clearly upregulated the expression of the HIF target gene EGLN3, while the upregulation effect on other HIF target genes such as SLC2A1, BNIP3, and EPO was relatively mild.
体内研究
(In Vivo)

ZG-2291 (10 mg/kg,腹腔注射,每隔一天一次,共 30 天) 可对抗 ob/ob 小鼠的肥胖症状,并显著改善其与肥胖相关的代谢功能障碍[1]

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

Animal Model: ob/ob mice
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.), every other day for a total of 30 days
Result: Resulted in lower body weight, reduced hepatic TG/TC, and lower serum TG/TC/low-density lipoprotein (LDL) cholesterol levels in mice compared to the control group
分子量

373.75

Formula

C17H12ClN3O5

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
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  • 稀释计算器

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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.

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ZG-2291
目录号:
HY-159120
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