產(chǎn)品目錄

規(guī)格	1mg 5mg 10mg 25mg
CAS	892549-43-8
別名	MF 63; MF-63
化學(xué)名	2-(9-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)isophthalonitrile
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
儲存條件	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

產(chǎn)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].

特別提醒：

1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

2. 為了您的安全和健康，請穿好實驗服并佩戴一次性手套和口罩操作。

原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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