产品说明
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.
基本信息
| 经验(实验)分子式 | C13H12ClN3O3S |
| 分子量 | 325.77 |
| MDL编号 | MFCD30533689 |
| NACRES | NA.77 |
产品性质
| 测定 | ≥98% (HPLC) |
| 形式 | powder |
| manufacturer/tradename | 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 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
