MF63

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MF63 是一种有效的、选择性的、口服活性的 mPGES-1 抑制剂，对人 mPGES-1 酶的 IC50 为 1.3 nM。

MF63 is a potent, selective, and orally active mPGES-1 inhibitor with IC50 of 1.3 nM for human mPGES-1 enzyme, >1000-fold selectivity over other prostanoid synthases; strongly inhibits guinea pig mPGES-1 (IC50= 0.9 nM) but not the mouse or rat enzyme; selectively suppresses the synthesis of PGE(2), but not other prostaglandins inhibitable by NSAIDs, yet retains NSAID-like efficacy at inhibiting LPS-induced pyresis, hyperalgesia, and iodoacetate-induced osteoarthritic pain, relieves pyresis and pain in preclinical models of inflammation.

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Animal Model:10 to 12 weeks of KI and wild-type mice which injected LPS.Dosage:10 mg/kg and 100 mg/kg.Administration:Oral gavage; single dose.Result:Inhibited the PGE2 accumulation in air pouch and brain of KI mice in a dose-dependent manner, and has selectively in the brain. Reduced the response of hyperalgesia by 50% at 10 mg/kg and 80% at 100 mg/kg in KI mice but without effecting wild-type mice.Animal Model:Young male Hartley guinea pigs (~250 g) with osteoarthritic pain.Dosage:0, 3, 10, 15, 30, 50, 100 or 150 mg/kg.Administration:Oral gavage; single dose.Result:Inhibited the formation of PGE2 in a dose-dependent manner, relieved Chronic Osteoarthritic-Like Pain and also inhibited pyresis.Animal Model:10 to 12 weeks of KI mice and nonhuman primates.Dosage:0, 3, 10, 30 or 100 mg/kg.Administration:Oral gavage; twice daily for 4 days.

MF 63 | MF-63

Immunology/Inflammation

PGE synthase

PGE synthase

Inflammation/Immunology

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892549-43-8

378.8

C23H11ClN4

>98% (HPLC)

DMSO: ≥ 43 mg/mL

N#CC1=CC=CC(C#N)=C1C2=NC3=C4C=CC(Cl)=CC4=C5C=CC=CC5=C3N2

1,3-Benzenedicarbonitrile, 2-(9-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)-

(-20℃)

With Ice Pack

≥ 2 years