PF-06869206

SKU: orb1296274

Description

PF-06869206

Research Area

Product Categories/Products/Small Molecules,Membrane transporter/Ion channel

Key Properties

• CAS Number: 2227425-05-8
• MW: 374.75
• Purity: 100%
• Formula: C₁₅H₁₄ClF₃N₄O₂
• SMILES: Cc1[nH]c2c(N3CCO[C@H](CO)C3)c(C#N)c(nc2c1Cl)C(F)(F)F

Bioactivity

• Target IC50:
  SLC34A1:380 nM
• 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)).
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• 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).
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• 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).
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Storage & Handling

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

Compound Identifiers

PubChem CID

134159047