| Name | PF-06869206 |
| Description | PF-06869206 is an oral selective inhibitor of the sodium-phosphate cotransporter NaPi2a (SLC34A1, IC50: 380 nM). |
| 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). |
| 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)). |
| 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.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (10.67 mM), Sonication is recommended.
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| Keywords | Sodiumdependentphosphatetransporter | Sodiumdependent phosphate transporter | SodiumChannel | Sodium Channel | SLC34A1 | PF-06869206 | PF06869206 | PF 06869206 | Na+ channels | Na channels | Inhibitor | inhibit |
| Inhibitors Related | Phenytoin sodium | Procaine | Lidocaine Hydrochloride hydrate | Lidocaine | Safinamide | Valproic Acid | Lidocaine hydrochloride | L-Aspartic aicd sodium | Mebeverine hydrochloride | Amitriptyline hydrochloride | Riluzole | Benzocaine |
| Related Compound Libraries | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Sodium Channel Targeted Library | Inhibitor Library | Neuroprotective Compound Library | Anti-Cardiovascular Disease Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Covalent Inhibitor Library | Ion Channel Targeted Library | Anti-Cancer Compound Library |
United States
