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Cat. No.: 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.

For research use only. We do not sell to patients.

CAS No.: 1795110-22-3
Formula: C₁₃H₉BrN₄O
Molecular Weight:317.14

Storage:

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

Data Sheet (277 KB)

ZG-2686 Chemical Structure

CAS No.: 1795110-22-3

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Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & TargetHIF-2α agonist

HIF-2α

0.25 μM (EC₅₀)

All HIF/HIF Prolyl-Hydroxylase Isoforms :

In Vitro

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

In Vivo

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.

Chemical Information

CAS No. 1795110-22-3
Molecular Weight 317.14
Formula C₁₃H₉BrN₄O
SMILES

O=C(NC1=NNC2=NC=CC=C21)C3=CC=C(Br)C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
COA (2659 KB)
Elemental Analysis Report (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)
Handling Instructions (2659 KB)

References

[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]

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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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