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PF-06282999
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产品介绍
产品介绍
产品信息
抗原名称
0
简单描述
PF06282999 是选择性的髓过氧物酶 (myeloperoxidase) 抑制剂，用于研究心血管疾病。
商品描述
PF-06282999 is a potent and selective myeloperoxidase inhibitor which is potentially useful for the treatment of cardiovascular diseases.
分子量
325.77
纯度
98.28%
性状
Solid
颜色
White
In vitro(体外研究)
The estimated EC50 for total 8 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.
In vivo(体内研究)
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. 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.
背景
别名
0
分子式
C13H12ClN3O3S
CAS号
1435467-37-0
密度
1.52 g/cm3 (Predicted)
制备和贮存
溶解方法
DMSO: 55 mg/mL (168.83 mM), Sonication is recommended.
存储溶液
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
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