PF-06282999，≥98% (HPLC)

图片 PF-06282999，≥98% (HPLC)
别名：PF 06282999, PF06282999；2-(6-(5-氯-2-甲氧基苯基)-4-氧代-2-硫代-3,4-二氢嘧啶-1(2H)-基)乙酰胺；6-（5-氯-2-甲氧基苯基）-3，4-二氢-4-氧代-2-硫代-1（2H）-嘧啶乙酰胺；2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide, 6-(5-Chloro-2-methoxyphenyl)-3,4-dihydro-4-oxo-2-thioxo-1(2H)-pyrimidineacetamide

Empirical Formula (Hill Notation): C13H12ClN3O3S CAS号: 1435467-37-0 分子量: 325.77 MDL编号: MFCD30533689 NACRES: NA.77
制造商品牌: 西格玛 Sigma-Aldrich
货号（SKU）: PZ0375
CAS号: 1435467-37-0
MDL号: MFCD30533689
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说明

生化/生理作用

PF-06282999 is an orally active thiouracil class myeloperoxidase (MPO) suicide substrate (kinact/KI = 11600 M-1s-1) that targets MPO heme group for mechanism-based irreversible inactivation wtih high selectivity over thyroid peroxidase (TPO kinact/KI <3 M-1s-1) and heme-containing cytochrome P450 (CYP) isoforms (IC50 >100 μM). PF-06282999 effectively inhibits MPO activity in human blood stimulated by LPS ex vivo (IC50 = 1.9 μM) and in blood of LPS-treated cynomolgus monkeys in vivo (5-80 mg/kg p.o. 1hr post LPS i.v.) with good pharmacokinetics and oral availability (100%/86%/75%/76% in mice/rats/dogs/monkeys). PF-06282999 also exhibits weak PXR activating activity (EC50/Emax = 279 μM/9.36-fold vs.0.8 μM/19.6-fold with rifampin).
 

法律信息

Sold for research purposes under agreement from Pfizer Inc
Pfizer is a registered trademark of Pfizer, Inc.
 
 

属性

测定

≥98% (HPLC)

形式

powder

mfr. no.

Pfizer®

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

创始人

Pfizer

储存温度

room temp

SMILES string

O=C(N)CN(C(N1)=S)C(C2=CC(Cl)=CC=C2OC)=CC1=O

 

安全信息

储存分类代码

13 - Non Combustible Solids

WGK

WGK 3

商品规格
属性名称属性值
储存温度 Storage temp.常温阴凉避光
全球实时库存 Availability √美国St. Louis ≥ 20 | 欧洲Eur. ≥ 16 | 東京Tokyo ≥ 5 | 香港与北京 ≥ 20
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