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PF-06282999
产品别名
1435467-37-0
PF-06282999
PF 06282999
PF06282999
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
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C13H12ClN3O3S |
| Molecular weight | 325.77 |
| MDL number | MFCD30533689 |
| NACRES | NA.77 |
| Biochem/physiol Actions【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). |
| Legal Information【法律信息】 | Sold for research purposes under agreement from Pfizer Inc Pfizer is a registered trademark of Pfizer, Inc. |
产品性质
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| manufacturer/tradename | Pfizer® |
| color【颜色】 | white to beige |
| solubility【溶解性】 | DMSO: 2 mg/mL, clear |
| originator【创始人】 | Pfizer |
| storage temp.【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
| Storage Class Code【储存分类代码】 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
