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Home > Inhibitors & Agonists > Membrane Transporter/Ion Channel > Sodium Channel

PF-06869206

  Cat. No.:  DC10834   Featured
Chemical Structure
2227425-05-8
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More than 5000 active chemicals with high quality for research!
Field of application
PF-06869206 is an Orally Bioavailable Selective Inhibitors of the Sodium-Phosphate Cotransporter NaPi2a (SLC34A1).
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2227425-05-8
Chemical Name: (S)-3-chloro-7-(2-(hydroxymethyl)morpholino)-2-methyl-5-(trifluoromethyl)-1H-pyrrolo[3,2-b]pyridine-6-carbonitrile
Synonyms: PF-06869206; PF 06869206; PF06869206
SMILES: N#CC1=C(C(F)(F)F)N=C2C(NC(C)=C2Cl)=C1N3C[C@@H](CO)OCC3
Formula: C15H14ClF3N4O2
M.Wt: 374.07
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: PF-06869206 is an orally bioavailable selective inhibitor of the sodium-phosphate cotransporter NaPi2a (SLC34A1) with an IC50 of 380 nM.
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), and rat liver microsome (RLM) clearance is low (<14 μL/min/mg; HLM=39 μL/min/mg)[1].
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[1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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