2. Metabolic Enzyme/Protease
  3. HIF/HIF Prolyl-Hydroxylase
  4. ZG-2686

ZG-2686 是一种强效的选择性 HIF-2α 激动剂，EC50 为 0.25 µM。ZG-2686 对 PHD2 具有选择性。ZG-2686 与 HIF-2α 的特定内部空腔结合，通过结构水分子形成氢键，从而稳定 HIF-2α/β 异二聚体并增强其转录活性。ZG-2686 与 Vadadustat (HY-101277) 具有协同作用，可在体外和体内上调 HIF-2α 依赖的 EPO 基因表达。ZG-2686 可用于肾性贫血的研究。

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ZG-2686

ZG-2686 Chemical Structure

CAS No. : 1795110-22-3

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ZG-2686 相关抗体

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HIF-1α HIF

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ZG-2686 is a potent and selective HIF-2α agonist with an EC50 of 0.25 µM. ZG-2686 exhibits selectivity over PHD2. ZG-2686 binds to a specific internal cavity of HIF-2α, forming hydrogen bonds via structural water molecules, which stabilizes the HIF-2α/β heterodimer and enhances transcriptional activity. ZG-2686 synergizes with Vadadustat (HY-101277) to upregulate HIF-2α-dependent EPO gene expression both in vitro and in vivo. ZG-2686 can be used for the research of renal anemia[1].

IC50 & TargetHIF-2α agonist

HIF-2α

0.25 μM (EC50)

体外研究
(In Vitro)

ZG-2686 在大鼠血浆和肝微粒体中表现出良好的体外代谢稳定性[1]。
ZG-2686 (10-20 μM；12 小时) 与 Vadadustat 联合使用时，可协同上调 Hep3B 细胞中 HIF-2α 依赖的 EPO mRNA 水平[1]。

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

ZG-2686 相关抗体:

Real Time qPCR[1]

Cell Line: Hep3B cells
Concentration: 10, 20 μM
Incubation Time: 12 h
Result: Had minimal effect on EPO mRNA level.
Produced a synergistic effect when combined with Vadadustat.
Increased EPO gene expression by 4.35-fold at 20 μM when combined with Vadadustat (20 μM).
体内研究
(In Vivo)

ZG-2686（10 和 20 mg/kg；腹腔注射；单次给药）单独在体内 EPO 诱导方面表现有限，但与 Vadadustat 协同作用可增强 C57BL/6 小鼠的 EPO 表达[1]。

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

Animal Model: Male C57BL/6 mice (6-8 weeks old, 18-22 g)[1]
Dosage: 10 and 20 mg/kg
Administration: i.p.; single dose
Result: Had minimal effect on EPO mRNA level.
Synergistically increased EPO gene expression when combined with the PHD inhibitor Vadadustat.
分子量

317.14

Formula

C13H9BrN4O
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

ZG-2686 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

ZG-26861795110-22-3ZG2686ZG 2686HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHVadadustatHIF-2α agonistProlyl hydroxylase domain inhibitorBifunctional codrugHIF-2αHIF-2α-dependent gene expressionRenal anemiaHIF-2Hypoxia-inducible factor-2PHD inhibitorCodrugEPOInhibitorinhibitorinhibit

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目录号：
HY-179647
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