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HNF4 agonist 46

Chemical Structure : HNF4 agonist 46

CAS No.:

HNF4 agonist 46

Catalog No.: PC-24565Not For Human Use, Lab Use Only.

HNF4 agonist 46 is a first-in-class, high-affinity hepatocyte nuclear factor 4 (HNF4) agonist, activates HNF4α (EC50=6 nM) and HNF4γ (EC50=17 nM) with low nanomolar potency, binds to HNF4α LBD with ITC Kd of 23 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

HNF4 agonist 46 is a first-in-class, high-affinity hepatocyte nuclear factor 4 (HNF4) agonist, activates HNF4α (EC50=6 nM) and HNF4γ (EC50=17 nM) with low nanomolar potency, binds to HNF4α LBD with ITC Kd of 23 nM.
HNF4 agonist 46 exhibits similar agonism on the highly related HNF4α and HNF4γ isoforms in cellular assays.
HNF4 agonist 46 displays favorable selectivity over other fatty acid/lipid sensing (THR, RAR, PPAR, VDR, LXR, FXR, RXR) and promiscuous (CAR, PXR) nuclear receptors at 1 uM.
HNF4 agonist 46 is a high-quality chemical tool to study HNF4 biology in vitro.

Physicochemical Properties

M.Wt 286.71
Formula C16H11ClO3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-[(2-Chloro-4-methylphenyl)ethynyl]-2-hydroxybenzoic Acid

References

1. Schallmayer E, et al. J Med Chem. 2025 May 8. doi: 10.1021/acs.jmedchem.5c00595.

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