PF06869206
- CAS NO.:2227425-05-8
- Empirical Formula: C15H14ClF3N4O2
- Molecular Weight: 374.75
- MDL number: MFCD31657405
- EINECS: 604-604-1
- Update Date: 2024-10-29 18:21:28
What is PF06869206?
Description
PF-06869206 is an orally bioavailable inhibitor of sodium-phosphate cotransporter 2a (NaPi2a; IC50 = 380 nM). It is selective for NaPi2a over NaPi2b, NaPi2c, PiT-1, and PiT-2 (IC50s = >25 μM).
Biological Activity
PF-06869206 (PF06869206) is a potent, selective, orally bioavailable inhibitor of sodium-phosphate cotransporter 2a (NaPi2a/SLC34A1) with IC50 of 380 nM, no inhibition against NaPi2b (SLC34A2) and NaPi2c (SLC34A3).PF-06869206 displays excellent subtype selectivity against other sodium-phosphate cotransporters: NaPi2b, NaPi2c, PiT-1, and PiT-2 (SLC20A2).PF-06869206 showed comparable submicromolar activity for the human, rat, and mouse NaPi2a isoforms (IC50=0.4-0.54 uM) and was selective over rodent NaPi2c, inhibited phosphate uptake in human proximal tubule cells.PF-06869206 was well tolerated and elicited a dose-dependent increase in fractional phosphate excretion, lowered plasma phosphate levels in WT mice and in rats with chronic kidney disease (CKD), induced an unabated acute phosphaturic and hypophosphatemic effect in CKD rats.
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.
Properties of PF06869206
Boiling point: | 599.2±50.0 °C(Predicted) |
Density | 1.57±0.1 g/cm3(Predicted) |
storage temp. | 2-8°C |
solubility | DMF: 1 mg/mL; DMSO: 1mg/mL; Ethanol: 10mg/mL; Ethanol:PBS (pH 7.2) (1:3): 0.25 mg/mL |
form | A crystalline solid |
pka | 11.78±0.40(Predicted) |
color | White to off-white |
Safety information for PF06869206
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P280:Wear protective gloves/protective clothing/eye protection/face protection. P301+P312:IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell. P302+P352:IF ON SKIN: wash with plenty of soap and water. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for PF06869206
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