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Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $33 | In Stock | |
10 mg | $58 | In Stock | |
25 mg | $127 | In Stock | |
50 mg | $221 | In Stock | |
100 mg | Inquiry | In Stock | |
1 mL x 10 mM (in DMSO) | $30 | In Stock |
Description | PF-06869206 is an oral selective inhibitor of the sodium-phosphate cotransporter NaPi2a (SLC34A1, IC50: 380 nM). |
Targets&IC50 | SLC34A1:380 nM |
In vitro | PF-06869206 (380 nM) shows NaPi2a inhibition potency. 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 (IC50s: 0.4 μM/0.54 μM for rat/mouse NaPi2a). |
In vivo | In rodent PK, PF-06869206 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)). |
Animal Research | Male Wistar-Han rats are treated with PF-06869206 (1 mg/kg, 5 mg/kg, and 50 mg/kg; 2 mL/kg for iv or 10 mL/kg for po) . C57BL6 mice are treated with PF-06869206 (1 mg/kg, 5 mg/kg, and 50 mg/kg; 2 mL/kg for iv or 10 mL/kg for po). |
Molecular Weight | 374.75 |
Formula | C15H14ClF3N4O2 |
Cas No. | 2227425-05-8 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 120 mg/mL (320.22 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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