货号	规格	价格	上海	北京	珠海	重庆	武汉
S83312-1mg买3赠1	98.50%	￥100.00 S83312-1mg ￥100.00 现货（买3赠1）	7 7	-	-	-	-
S83312-5mg买3赠1	98.50%	￥132.00 S83312-5mg ￥132.00 现货（买3赠1）	13 >10	-	-	-	-
S83312-10mg买3赠1	98.50%	￥255.00 S83312-10mg ￥255.00 现货（买3赠1）	9 9	-	-	-	-
S83312-25mg买3赠1	98.50%	￥370.00 S83312-25mg ￥370.00 现货（买3赠1）	4 4	-	-	-	-
S83312-50mg	98.50%	￥710.00 S83312-50mg ￥710.00 现货	4 4	-	-	-	-
S83312-100mg	≥98%	￥1040.00 S83312-100mg ￥1040.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

PF-06282999 is a potent and selective myeloperoxidase inhibitor which is potential useful for the treatment of cardiovascular diseases.

靶点：

GlutathionePeroxidase

体外研究：

PF-06282999 (Compound 8) is a potent and selective myeloperoxidase inhibitor. The estimated EC50 for total PF-06282999 concentration in plasma is 3.8 μM, which corresponds well with the IC50 value obtained in the human whole blood assay of 1.9 μM

体内研究：

PF-06282999 is moderately bound to plasma proteins across preclinical species and humans. The blood/plasma ratios for PF-06282999 are 1.1, 1.1, 0.91, 1.2, and 0.94 in mice, rats, dogs, monkeys, and humans, respectively, suggesting that PF-06282999 is equally distributed into plasma and red blood cells. The in vivo pharmacokinetics of PF-06282999 are examined in greater detail in mice, rats, dogs, and monkeys, wherein it is demonstrated to have low CLp in mice (10.1 mL/min/kg), dogs (3.39 mL/min/kg), monkeys (10.3 mL/min/kg) and moderate CLp in rats (41.8 mL/min/kg). The terminal plasma elimination half-lives (t1/2) range from 0.75 to 3.3 h in the four species. Approximately 26-32% of the iv dose of PF-06282999 is excreted in the unchanged form in rat, dog, and monkey urine, wherein it is also shown that it is well distributed with steady state distribution volumes (Vdss) ranging from 0.5-2.1 L/kg in mice, rats, dogs, and monkeys. Following oral administration, PF-06282999 is rapidly (Tmax=0.78-1.70 h) and well absorbed in mice, rats, dogs, and monkeys with oral bioavailability values of 100%, 86%, 75%, and 76%, respectively

参考文献：

1. Dong JQ, et al. Pharmacokinetics and Disposition of the Thiouracil Derivative PF-06282999, an Orally Bioavailable, Irreversible Inactivator of Myeloperoxidase Enzyme, Across Animals and Humans. Drug Metab Dispos. 2016 Feb;44(2):209-19. 2. Ruggeri RB, et al. Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases. J Med Chem. 20

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	3.07 ml	15.348 ml	30.696 ml
5 mM	0.614 ml	3.07 ml	6.139 ml
10 mM	0.307 ml	1.535 ml	3.07 ml
50 mM	0.061 ml	0.307 ml	0.614 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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