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ZG-2686 is a potent and selective agonist of HIF-2α with an EC50 of 0.25 µM, demonstrating selectivity for PHD2. It binds to a specific internal cavity of HIF-2α, forming hydrogen bonds through structural water molecules, which stabilizes the HIF-2α/β heterodimer and enhances its transcriptional activity. The compound acts synergistically with Vadadustat to upregulate HIF-2α-dependent EPO gene expression both in vitro and in vivo. ZG-2686 is applicable for renal anemia research.
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | ZG-2686 is a potent and selective agonist of HIF-2α with an EC50 of 0.25 µM, demonstrating selectivity for PHD2. It binds to a specific internal cavity of HIF-2α, forming hydrogen bonds through structural water molecules, which stabilizes the HIF-2α/β heterodimer and enhances its transcriptional activity. The compound acts synergistically with Vadadustat to upregulate HIF-2α-dependent EPO gene expression both in vitro and in vivo. ZG-2686 is applicable for renal anemia research. |
| Targets&IC50 | HIF2α:0.25 μM (EC50) |
| In vitro | ZG-2686 demonstrates excellent in vitro metabolic stability in rat plasma and liver microsomes. When combined with Vadadustat (10-20 μM; 12 hours), ZG-2686 synergistically enhances the levels of HIF-2α-dependent EPO mRNA in Hep3B cells. |
| In vivo | ZG-2686 (10 and 20 mg/kg; intraperitoneal injection; single dose) shows limited efficacy in inducing EPO on its own in vivo, but it can enhance EPO expression in C57BL/6 mice when used in synergy with Vadadustat. |
| Molecular Weight | 317.15 |
| Formula | C13H9BrN4O |
| Cas No. | 1795110-22-3 |
| Smiles | O=C(NC1=NNC=2N=CC=CC21)C3=CC=C(Br)C=C3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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