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PF-06869206 is an oral selective inhibitor of the sodium-phosphate cotransporter NaPi2a (SLC34A1, IC50: 380 nM).

| 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 | Preferential | 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 |
| Smiles | Cc1[nH]c2c(N3CCO[C@H](CO)C3)c(C#N)c(nc2c1Cl)C(F)(F)F |
| Relative Density. | 1.57 g/cm3 (Predicted) |
| Color | White |
| Appearance | Solid |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 120 mg/mL (320.21 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (10.67 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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