Biochem/physiol Actions
PF-06752469 (PF-6752469) is an orally active, non-cytotoxic (300 μM, HepG2), potent and selective ketohexokinase (KHK) inhibitor (human KHK-A/C IC50 = 390/450 nM; rat KHK IC50 = 340 nM) with no significant activity against a broad panel of transporters, receptors, ion channels, and enzymes, including hERG and human CYP450s. PF-06752469 prevents fructose administration-induced fructose 1-phosphate (F1P) upregulation (hepatic/renal ED50 = 15.7/30.0 mg/kg p.o. 2 min prior to 500 mg fructose/10 mL/kg i.v. in rats) by inhibiting KHK-mediated fructose metabolism in vivo.
- UPC:
- 51283709
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- PZ0417-25MG
- Product Size:
- 25/MG
- CAS:
- 2135304-43-5