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Chemical Structure : mPGES-1 inhibitor UK-4b
Catalog No.: 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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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.
| M.Wt | 404.89 | |
| Formula | C21H25ClN2O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Kai Ding, et al. Sci Rep. 2018 Mar 26;8(1):5205.
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