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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Sodium Channel-PF-06869206
PF-06869206

Chemical Structure : PF-06869206

CAS No.: 2227425-05-8

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PF-06869206 (PF06869206)

货号: 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 ￥780 In stock
10 mg ￥1180 In stock
25 mg ￥2180 In stock
50 mg ￥3580 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 374.748
分子式 C15H14ClF3N4O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
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

参考文献

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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