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

ZG-2686

ZG-2686 Chemical Structure

CAS No. : 1795110-22-3

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Description

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)

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.

ZG-2686 Related Antibodies

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 Tmax Cmax AUC0-t AUC0-∞ T1/2 CL Vz MRT0-∞
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.
Molecular Weight

317.14

Formula

C13H9BrN4O
CAS No.
SMILES

O=C(NC1=NNC2=NC=CC=C21)C3=CC=C(Br)C=C3
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ZG-2686 Related Classifications

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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:

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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