PF-06835919 | Ketohexokinase inhibitor

CAS:
 2102501-84-6
Catalog Number:
 10-3958
PF-06835919 chemical structure

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1 mg$80.00
5 mg$295.00

PF-06835919 (2102501-84-6) is a potent (IC50 = 10 nM KHK-C; 170 nM KHK-A) inhibitor of ketohexokinase (KHK), the first enzyme in the fructose metabolic cascade.1 It displayed high selectivity against other sugar kinases. PF-06835919 prevented hyperinsulinemia, hypertriglyceridemia, and hepatic steatosis in fructose-fed rats.2 The increased tumor proliferation effect of fructose in CaSki cells was inhibited by PF-06835919.3 An interesting new tool to study metabolic and fatty liver diseases.

References/Citations:

  1. Futatsugi et al. (2020), Discovery of PF-06835919: A Potent Inhibitor of Ketohexokinase (KHK) for the Treatment of Metabolic Disorders Driven by the Overconsumption of Fructose; J. Med. Chem. 63 13546
  2. Gutierrez et al. (2021), Pharmacologic inhibition of ketohexokinase prevents fructose-induced metabolic dysfunction; Mol. Metab. 48 101196
  3. Fowle-Girder et al. (2024), Dietary fructose enhances tumour growth indirectly via interorgan lipid transfer; Nature 636 737
CAS:
2102501-84-6
Catalog Number:
10-3958
Activity:
Ketohexokinase inhibitor
Chemical Names:
2-[(1R,5S)-3-[2-[(2S)-2-methylazetidin-1-yl]-6-(trifluoromethyl)pyrimidin-4-yl]-3-azabicyclo[3.1.0]hexan-6-yl]acetic acid
Molecular Weight:
356.35
Molecular Formula:

C16H19F3N4O2

Solubility:
Soluble in DMSO (10 mg/ml with warming)
Physical Properties:
White solid
Purity:

>98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

Product Data Sheet:

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