Formulation: A solid
Formal Name: (1α,5α,6α)-3-[2-[(2S )-2-methyl-1-azetidinyl]-6-(trifluoromethyl)-4-pyrimidinyl]-3-azabicyclo[3.1.0]hexane-6-acetic acid
Purity: ≥98%
Formula Markup: C16H19F3N4O2
Formula Weight: 356,3
Shelf life (days): 1460
CAS Number: 2102501-84-6
Notes: PF-06835919 is an inhibitor of ketohexokinase C (KHK-C; IC50 = 10 nM).{66932} It is selective for KHK-C over KHK-A (IC50 = 170 nM) and a panel of 89 kinases, phosphatases, and receptors at 10 µM. PF-06835919 decreases the levels of fructose-1-phosphate in primary human- and rat hepatocytes (IC50s = 0.232 and 2.801 µM, respectively).{66933} It inhibits glucose- and fructose-induced nuclear translocation of carbohydrate-responsive element-binding protein (ChREBP) in a reporter assay using primary rat hepatocytes when used at a concentration of 30 µM. PF-06835919 (10 or 30 mg/kg twice per day) reduces the weight of epididymal adipose tissue, fasting plasma levels of insulin, hepatic levels of triglycerides, and fed- and fasting plasma levels of triglycerides and increases urinary levels of fructose in rats fed a high-fructose diet. It decreases plasma levels of apolipoprotein C3 (ApoC3) and increases plasma levels of adiponectin in rats fed a Western diet when administered at doses of 20 or 60 mg/kg per day.
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