PF-06869206 |
Catalog No.GC19289 |
PF-06869206 est un inhibiteur sélectif biodisponible par voie orale du cotransporteur de phosphate de sodium NaPi2a (SLC34A1) avec une IC50 de 380 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2227425-05-8
Sample solution is provided at 25 µL, 10mM.
PF-06869206 is an orally bioavailable selective inhibitor of the sodium-phosphate cotransporter NaPi2a (SLC34A1) with an IC50 of 380 nM.
PF-06869206 shows a balance of attributes with 380 nM NaPi2a inhibition potency, excellent subtype selectivity, and acceptable aqueous solubility (46 uM). PF-06869206 is profiled for potency in the rodent NaPi2a and NaPi2c cell lines. PF-06869206 shows comparable submicromolar activity for the human, rat, and mouse NaPi2a isoforms with IC50s of 0.4±0.047 uM and 0.54±0.099 uM for rat NaPi2a and mouse NaPi2a, respectively[1].
PF-06869206 is evaluated in rodent PK studies to determine suitability for in vivo pharmacology exploration. Results show moderate clearance in both rat and mouse. Oral bioavailability at 5 mg/kg is good in rat and moderate in mouse. At higher oral doses of 50 mg/kg, supraproportional increases in exposure are observed in both species, suggestive of saturation of clearance. PF-06869206 has moderate terminal elimination half-life (t1/2=1.35 h, and 0.75 h for Wistar-Han rats (10 mg/kg, iv), and C57BL6 mice (1 mg/kg, iv)). Furthermore, permeability is good (14×10-6 cm/s), and rat liver microsome (RLM) clearance is low (<14 uL/min/mg; HLM=39 uL/min/mg)[1].
References:
[1]. Filipski KJ, et al. Discovery of Orally Bioavailable Selective Inhibitors of the Sodium-Phosphate Cotransporter NaPi2a (SLC34A1). ACS Med Chem Lett. 2018 Apr 12;9(5):440-445.
Average Rating: 5
(Based on Reviews and 29 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *