PF-06869206

SKU: orb1218407

Description

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

Key Properties

• CAS Number: 2227425-05-8
• MW: 374.75
• Purity: >98% (HPLC)
• Formula: C₁₅H₁₄ClF₃N₄O₂
• SMILES: CC1=C(C2=C(N1)C(=C(C(=N2)C(F)(F)F)C#N)N3CCO[C@@H](C3)CO)Cl
• Target: Sodium Channel
• Solubility: DMSO:120 mg/mL (320.22 mM)

Bioactivity

• In Vivo:
  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), andrat liver microsome (RLM) clearance is low (<14 μL/min/mg; HLM = 39 μL/min/mg).
• In Vitro:
  PF-06869206 shows a balance of attributes with 380 nM NaPi2a inhibition potency, excellent subtype selectivity, and acceptable aqueous solubility (46 μM). 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 μM and 0.54±0.099 μM for rat NaPi2a and mouse NaPi2a, respectively.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Sodium Channel