| Bioactivity | MF63 is a selective and orally active inhibitor of mPGES-1. MF63 reduces the accumulation of PGE2, relieves pyresis, hyperalgesia, and inflammatory pain by inhibiting mPGES-1[1]. | ||||||||||||
| Target | mPGES-1 | ||||||||||||
| Invitro | MF63 (0.01-100 µM；24 h) 选择性抑制 A549 细胞中 10 ng/mL IL-1β 诱导的 PGE2 生成，并以剂量依赖的方式增加 PGF2α 的形成[1]。MF63 (10 µM；24 h) 增强了多种金属硫蛋白 1 (MT1) 亚型以及 IL-1 和 IL-36 的内源性拮抗剂的表达，具有抗炎作用[2]。 | ||||||||||||
| In Vivo | MF63 (100 mg/kg；口服；单剂量) 可减少 KI (敲入 mPGES-1 基因) 小鼠气囊和大脑中 PEG2 的积累，并以剂量依赖的方式抑制 PEG2 的形成[1]。MF63 (10 mg/kg 和 100 mg/kg；口服；单剂量) 以剂量依赖的方式抑制 KI 小鼠中 LPS 诱导的痛觉过敏反应[1]。MF63 (0-150 mg/kg；口服；单剂量) 抑制豚鼠中 PEG2 合成、痛觉过敏、发热，并缓解慢性骨关节炎样疼痛[1]。MF63 (0-100 mg/kg；口服；每天两次，共 4 天) 对 KI 小鼠和非人类灵长类动物具有胃肠耐受性[1]。 Animal Model: | ||||||||||||
| Name | MF63 | ||||||||||||
| CAS | 892549-43-8 | ||||||||||||
| Formula | C23H11ClN4 | ||||||||||||
| Molar Mass | 378.81 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Xu D, et al. MF63 [2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)-isophthalonitrile], a selective microsomal prostaglandin E synthase-1 inhibitor, relieves pyresis and pain in preclinical models of inflammation. J Pharmacol Exp Ther. 2008 Sep;326(3):754-63. [2]. Tuure L, et al. Regulation of gene expression by MF63, a selective inhibitor of microsomal PGE synthase 1 (mPGES1) in human osteoarthritic chondrocytes. Br J Pharmacol. 2020 Sep;177(18):4134-4146. |