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PF-06869206

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Purity:100%

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COA HNMR LCMS

PF-06869206

Catalog No. TQ0011Cas No. 2227425-05-8

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

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Pack Size	Price	Availability
5 mg	$33	In Stock
10 mg	$58	In Stock
25 mg	$127	In Stock
50 mg	$221	In Stock
100 mg	Inquiry	In Stock
1 mL x 10 mM (in DMSO)	$30	In Stock

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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 Weight	374.75
Formula	C15H14ClF3N4O2
Cas No.	2227425-05-8

Storage & Solubility Information

Storage

Powder: -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

	1mg	5mg	10mg	50mg
1 mM	2.6684 mL	13.3422 mL	26.6845 mL	133.4223 mL
5 mM	0.5337 mL	2.6684 mL	5.3369 mL	26.6845 mL
10 mM	0.2668 mL	1.3342 mL	2.6684 mL	13.3422 mL
20 mM	0.1334 mL	0.6671 mL	1.3342 mL	6.6711 mL
50 mM	0.0534 mL	0.2668 mL	0.5337 mL	2.6684 mL
100 mM	0.0267 mL	0.1334 mL	0.2668 mL	1.3342 mL

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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