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製品番号: HY-179647

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ZG-2686

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 1795110-22-3
分子式: C₁₃H₉BrN₄O
分子量:317.14

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (277 KB)

ZG-2686 構造式

CAS 番号: 1795110-22-3

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- Parmacokinetics
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & TargetHIF-2α agonist

HIF-2α

0.25 μM (EC₅₀)

HIF/HIF Prolyl-Hydroxylase アイソフォーム固有の製品をすべて表示 :

体外実験

ZG-2686 demonstrates good in vitro metabolic stability in rat plasma and liver microsomes^[1].
ZG-2686 (10-20 μM; 12 h) shows a synergistic upregulation of HIF-2α-dependent EPO mRNA level in Hep3B cells when combined with Vadadustat^[1].

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

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).

Parmacokinetics

Species	Dose	Route	T_max	C_max	AUC_0-t	AUC_0-∞	T_1/2	CL	V_z	MRT_0-∞
Rat^[1]	1 mg/kg	i.v.	0.083 h	226.1 ng/mL	102.3 ng·h/mL	111.9 ng·h/mL	0.27 h	4614.2 mL/h/kg	1783.7 mL/kg	0.36 h
Rat^[1]	50 mg/kg	i.p.	2.67 h	1761.6 ng/mL	10143.0 ng·h/mL	11352.2 ng·h/mL	9.03 h	2220.1 mL/h/kg	27830.4 mL/kg	6.77 h

体内実験

ZG-2686 (10 and 20 mg/kg; i.p.; single dose) shows limited in vivo EPO induction alone but synergizes with Vadadustat to enhance EPO expression in C57BL/6 mice^[1].

MedChemExpress (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.

化学情報

CAS 番号 1795110-22-3
分子量 317.14
分子式 C₁₃H₉BrN₄O
SMILES

O=C(NC1=NNC2=NC=CC=C21)C3=CC=C(Br)C=C3
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (277 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Gao Y, et al. Discovery of 3-(Arylamido)pyrazolopyridine HIF-2α Agonists and a Codrug Strategy with Prolyl Hydroxylase Inhibition for Synergistic Treatment of Renal Anemia. J Med Chem. 2025;68(23):25569-25589. [Content Brief]

Calculators

モル濃度計算機

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

Mass Mass

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分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

100 mg

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