PF-06282999

产品名称：

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

产品介绍：

产品说明

生化/生理作用

PF-06282999 is an orally active thiouracil class myeloperoxidase (MPO) suicide substrate (k_inact/K_I = 11600 M^-1s^-1) that targets MPO heme group for mechanism-based irreversible inactivation wtih high selectivity over thyroid peroxidase (TPO k_inact/K_I <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