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.
Biological Activity
Description
IC50 & Target
HIF-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. Further protocols information, click here.
-
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
In Vivo
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.
Protocols
-
RT-PCR
Reverse transcription technology uses RNA as a template to synthesize DNA. RT-PCR is simple, specific and sensitive, and can be used to detect gene expression levels and expression differences in cells; detect RNA virus content; clone cDNA sequences of specific genes.
-
Dual Luciferin reporter gene assay
Luciferin reporter gene assay is a reporting system to detect the activity of Firefly Luciferase using luciferin as a substrate, which is often used in the research of miRNA target gene verification and promoter transcriptive activity regulation. Dual luciferase usually refers to Firefly luciferase and Renilla luciferase.
-
RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
-
Real Time qPCR (Q-PCR)
Real-time quantitative PCR (qPCR) quantifies an amplifiable nucleic-acid target by monitoring fluorescence during PCR cycling rather than measuring product only after amplification. The increase in fluorescence tracks accumulation of PCR product, and the quantification cycle (Cq; historically also Ct/CP) is related to the initial amount of target: samples containing more starting target generally reach the defined fluorescence threshold in fewer cycles.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)