货号	规格	价格	上海	北京	珠海	重庆	武汉
S88603-5mg促销	98%	￥750.00 ￥590.00 S88603-5mg ￥590.00 现货	10 10	-	-	-	-
S88603-10mg促销	98%	￥1200.00 ￥950.00 S88603-10mg ￥950.00 现货	7 7	-	-	-	-
S88603-25mg促销	98%	￥2400.00 ￥1910.00 S88603-25mg ￥1910.00 现货	3 3	-	-	-	-
S88603-50mg促销	98%	￥3900.00 ￥3110.00 S88603-50mg ￥3110.00 现货	1 1	-	-	-	-

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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

靶点：

IC50: 380 nM (NaPi2a/SLC34A1);SodiumChannel

体外研究：

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

体内研究：

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)

参考文献：

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.

溶解性：

Soluble in DMSO

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.668 ml	13.342 ml	26.684 ml
5 mM	0.534 ml	2.668 ml	5.337 ml
10 mM	0.267 ml	1.334 ml	2.668 ml
50 mM	0.053 ml	0.267 ml	0.534 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

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PF-06869206

PF06869206

参考文献

质检证书(COA)

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)