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PF-06869206

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Catalog No. TQ0011Cas No. 2227425-05-8

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

PF-06869206

PF-06869206

🥰Excellent
Purity: 99.79%
Catalog No. TQ0011Cas No. 2227425-05-8
PF-06869206 is an oral selective inhibitor of the sodium-phosphate cotransporter NaPi2a (SLC34A1, IC50: 380 nM).
Pack SizePriceAvailabilityQuantity
5 mg31 €In Stock
10 mg55 €In Stock
25 mg120 €In Stock
50 mg209 €In Stock
100 mgInquiryIn Stock
1 mL x 10 mM (in DMSO)28 €In Stock
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Purity:99.79%
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Product Introduction

Bioactivity
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).
Chemical Properties
Molecular Weight374.75
FormulaC15H14ClF3N4O2
Cas No.2227425-05-8
SmilesCc1[nH]c2c(N3CCO[C@H](CO)C3)c(C#N)c(nc2c1Cl)C(F)(F)F
Relative Density.1.57 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.6684 mL13.3422 mL26.6845 mL133.4223 mL
5 mM0.5337 mL2.6684 mL5.3369 mL26.6845 mL
10 mM0.2668 mL1.3342 mL2.6684 mL13.3422 mL
20 mM0.1334 mL0.6671 mL1.3342 mL6.6711 mL
50 mM0.0534 mL0.2668 mL0.5337 mL2.6684 mL
100 mM0.0267 mL0.1334 mL0.2668 mL1.3342 mL

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