mPGES-1 inhibitor UK-4b

Chemical Structure : mPGES-1 inhibitor UK-4b

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货号: PC-20005Not For Human Use, Lab Use Only.

mPGES-1 inhibitor UK-4b is a potent, hgihly selective and orally bioavailable inhibitor of human and mouse mPGES-1 enzymes with IC50 of 33 and 157 nM, respectively, effectively decreases carrageenan-stimulated PGE2 over-production.

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生物&药学活性

mPGES-1 inhibitor UK-4b is a potent, hgihly selective and orally bioavailable inhibitor of human and mouse mPGES-1 enzymes with IC50 of 33 and 157 nM, respectively, effectively decreases carrageenan-stimulated PGE2 over-production.
UK4b is highly selective for mPGES-1 over COX-1/2 (IC50 values >50 uM).
UK4b administered with low dose (0.1 mg/kg, s.c.) significantly decreased the PGE2 levels in mice, and (1 mg/kg, s.c.) reached the ceiling for decreasing the PGE2 level through the complete mPGES-1 inhibition.
UK4b decreasd the PGE2 (an inflammatory marker) levels compared to the currently available drug celecoxib in vivo.
mPGES-1 inhibitor UK-4b (10 mg/kg) exhibited anti-inflammatory and analgesic effects on carrageenan-induced paw edema and hyperalgesia, adjuvant-induced knee joint arthritis, and mouse model of postoperative pain.

物理化学性质&存储条件

分子量	404.89
分子式	C21H25ClN2O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	5-(3-chloro-4-(4-cyclohexylbutoxy)benzylidene)pyrimidine-2,4,6(1H,3H,5H)-trione

参考文献

1. Kai Ding, et al. Sci Rep. 2018 Mar 26;8(1):5205.