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PF-06869206 Sale

目录号 : GC19289

An NaPi2a inhibitor

PF-06869206 Chemical Structure

Cas No.:2227425-05-8

规格 价格 库存 购买数量
5mg
¥828.00
现货
10mg
¥1,332.00
现货
25mg
¥2,700.00
现货
50mg
¥4,320.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Animal experiment:

Rats and Mice[1]Male Wistar-Han rats (n=2) 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 (n=2) 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) [1].

References:

[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.

产品描述

PF-06869206 is an orally bioavailable selective inhibitor of the sodium-phosphate cotransporter NaPi2a (SLC34A1) with an IC50 of 380 nM.

PF-06869206 shows a balance of attributes with 380 nM NaPi2a inhibition potency, excellent subtype selectivity, and acceptable aqueous solubility (46 uM). 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 uM and 0.54±0.099 uM for rat NaPi2a and mouse NaPi2a, respectively[1].

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 uL/min/mg; HLM=39 uL/min/mg)[1].

References:
[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.

Chemical Properties

Cas No. 2227425-05-8 SDF
Canonical SMILES ClC1=C(C)NC2=C(N3C[C@@H](CO)OCC3)C(C#N)=C(C(F)(F)F)N=C21
分子式 C15H14ClF3N4O2 分子量 374.75
溶解度 DMSO : ≥ 125 mg/mL (333.56 mM) 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.6684 mL 13.3422 mL 26.6845 mL
5 mM 0.5337 mL 2.6684 mL 5.3369 mL
10 mM 0.2668 mL 1.3342 mL 2.6684 mL
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