CAS NO: | 892549-43-8 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
Cas No. | 892549-43-8 |
别名 | 2-(9-氯-1H-菲并[9,10-D]咪唑-2-基)-1,3-苯二甲腈,MF 63; MF-63 |
化学名 | 2-(9-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)isophthalonitrile |
Canonical SMILES | ClC1=CC(C2=CC=CC=C2C3=C4NC(C5=C(C#N)C=CC=C5C#N)=N3)=C4C=C1 |
分子式 | C23H11ClN4 |
分子量 | 378.81 |
溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml |
储存条件 | Store at -20℃ |
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 | IC50: 0.9 and 1.3 nM for pig mPGES-1 and human mPGES-1 MF63 is a potent, selective and orally active mPGES-1 inhibitor. Microsomal prostaglandin E synthase-1 (mPGES-1) is a terminal prostaglandin E2 synthase in the cyclooxygenase pathway. Thus, inhibitors of mPGES-1 may block prostaglandin E2 production and relieve inflammatory symptoms. In vitro: MF63 was found to be significantly more potent than those previously reported mPGES-1 inhibitors with an intrinsic inhibitory potency on the recombinant human mPGES-1 enzyme. Furthermore, MF63 showed a PGE2 whole cell inhibition in A549 cells and a human whole blood activity [1]. In vivo: In rodent species, MF63 inhibited guinea pig mPGES-1 strongly but not the mouse or rat enzyme. When tested in the guinea pig and a knock-in (KI) mouse expressing human mPGES-1, MF63 suppressed the synthesis of PGE2 selectively, but not other prostaglandins that were inhibitable by nonsteroidal anti-inflammatory drugs (NSAID), yet remaided NSAID-like efficacy at inhibiting lipopolysaccharide-induced hyperalgesia, pyresis, and iodoacetate-induced osteoarthritic pain. Additionally, MF63 did not cause NSAID-like gastrointestinal toxic effects, such as mucosal erosions or leakage in the KI mice or nonhuman primates, although MF63 markedly inhibited PGE2 synthesis in the KI mouse stomach [1]. Clinical trial: N/A Reference: |