| Cas No. | 1268709-57-4 |
| 化学名 | N-cyclopentyl-1-[5,6-dimethyl-1-(1-methylethyl)-1H-benzimidazol-2-yl]-4-piperidinecarboxamide |
| Canonical SMILES | O=C(C1CCN(C2=NC3=CC(C)=C(C)C=C3N2C(C)C)CC1)NC4CCCC4 |
| 分子式 | C23H34N4O |
| 分子量 | 382.5 |
| 溶解度 | DMF: 15 mg/ml,DMSO: 5 mg/ml,Ethanol: 25 mg/ml,Ethanol:PBS (pH 7.2) (1:8): 0.1 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product PGH2 into the biologically active PGE2. Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1β, and TNF-α. CAY10678 is a benzoimidazole that potently inhibits human and rat recombinant mPGES-1 (IC50 = 0.09 and 0.9 uM, respectively). It has minimal effects on COX-1, COX-2, PGIS, and hematopoietic PGDS at 50 μM but reduces lipocalin-type PGDS activity by 60% at this concentration. CAY10678 dose-dependently blocks PGE2 synthesis in isolated cells and whole blood treated with LPS or IL-1β. It also dose-dependently reduces PGE2 synthesis and cell recruitment during inflammation in mice. |
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