PF-06869206 | NaPi2a inhibitor | Probechem Biochemicals

Chemical Structure : PF-06869206

CAS No.: 2227425-05-8

PF-06869206 (PF06869206)

Catalog No.: PC-35086Not For Human Use, Lab Use Only.

PF-06869206 (PF06869206) is a novel potent, selective, orally bioavailable inhibitor of Sodium-Phosphate Cotransporter NaPi2a (SLC34A1) with IC50 of 380 nM.

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5 mg	$78	In stock
10 mg	$118	In stock
25 mg	$218	In stock
50 mg	$358	In stock
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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.

Physicochemical Properties

M.Wt	374.748
Formula	C15H14ClF3N4O2
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-3-chloro-7-(2-(hydroxymethyl)morpholino)-2-methyl-5-(trifluoromethyl)-1H-pyrrolo[3,2-b]pyridine-6-carbonitrile

References

1. Kevin J. Filipski, et al. ACS Med. Chem. Lett., 2018, 9 (5), pp 440-445.
2. Clerin V, et al. J Clin Invest. 2020 Dec 1;130(12):6510-6522.
3. Thomas L, et al. Am J Physiol Renal Physiol. 2020 Sep 1;319(3):F541-F551.

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PF-06869206 (PF06869206)

Biological Activity

Physicochemical Properties

References

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