貨號	規(guī)格	價格	上海	北京	武漢	南京
S83312-1mg	98.5%	￥100.00 S83312-1mg ￥100.00 現(xiàn)貨	7 7	-	-	-
S83312-5mg	98.5%	￥138.00 S83312-5mg ￥138.00 現(xiàn)貨	14 >10	-	-	-
S83312-25mg	98.5%	￥470.00 S83312-25mg ￥470.00 現(xiàn)貨	4 4	-	-	-
S83312-50mg	98.5%	￥790.00 S83312-50mg ￥790.00 現(xiàn)貨	4 4	-	-	-
S83312-100mg	≥98%	￥1350.00 S83312-100mg ￥1350.00 2-3天	0 貨期：2-3天	-	-	-
S83312-10mg	98.5%	￥2570.00 S83312-10mg ￥2570.00 現(xiàn)貨	10 10	-	-	-

產品介紹

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

產品描述：

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

靶點：

GlutathionePeroxidase

體外研究：

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

體內研究：

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

參考文獻：

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

保存條件：

-20℃

配置溶液濃度參考：

	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：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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