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PF-06869206

Catalog No. TQ0011 CAS 2227425-05-8

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

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PF-06869206, CAS 2227425-05-8

Pack Size	Availability	Price/USD
2 mg	In stock	$ 34.00
5 mg	In stock	$ 55.00
10 mg	In stock	$ 97.00
25 mg	In stock	$ 213.00
50 mg	In stock	$ 369.00
100 mg	In stock	$ 549.00
1 mL * 10 mM (in DMSO)	In stock	$ 45.00

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Purity: 100%

Biological Description

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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).

Molecular Weight	374.75
Formula	C15H14ClF3N4O2
CAS No.	2227425-05-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 120 mg/mL (320.22 mM)

References and Literature

1. Filipski KJ, et al. Discovery of Orally Bioavailable Selective Inhibitors of the Sodium-Phosphate Cotransporter NaPi2a (SLC34A1). ACS Med Chem Lett. 2018 Apr 12;9(5):440-445.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Ion Channel Inhibitor Library Bioactive Compounds Library Max Sodium Channel Blocker Library NO PAINS Compound Library Anti-Cancer Compound Library Bioactive Compound Library Anti-Cardiovascular Disease Compound Library Orally Active Compound Library

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Keywords

PF-06869206 2227425-05-8 Membrane transporter/Ion channel Sodium Channel PF 06869206 inhibit Na+ channels PF06869206 Na channels Inhibitor inhibitor

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