| Bioactivity | MF498 is a selective and orally active E prostanoid Receptor 4 (EP4) antagonist with a Ki value of 0.7 nM. MF498 can be used in the research of inflammation, such as rheumatoid and osteoarthritis[1][2]. | ||||||||||||
| Invitro | MF498(0.01 nM-10 μM，30 分钟) 抑制 PGE2 刺激的 cAMP 积累，在存在和不存在 10% 血清的情况下，IC50 值分别为 1.7 和 17 nM[1] .MF498 0.01 和 0.1 μM，30 分钟) 抑制大鼠 VSMC 中 FBS 和 PDGF-BB 诱导的 VSMC 增殖[2]。MF498 (0.1 μM，30 分钟) 降低大鼠 VSMC 中 PDGF 诱导的细胞周期蛋白 D1 和 PCNA 表达[2]。MF498 (0.1 μM，30 分钟) 抑制 PDGF-BB 诱导的迁移[2]。 Cell Viability Assay[2] Cell Line: | ||||||||||||
| In Vivo | MF498 (0-20 mg/kg，口服) 抑制佐剂性关节炎 (AIA) 大鼠的爪肿胀[1]。MF498 (0-30 mg/kg，口服) 减轻豚鼠中 EP4 激动剂 (L-902688) 诱导的痛觉过敏[1]。MF498 (20 mg/kg，口服) 显示出 100% 的生物利用度，给药后 6 小时的血浆浓度为 1.2 μM[1]。 Animal Model: | ||||||||||||
| Name | MF498 | ||||||||||||
| CAS | 915191-42-3 | ||||||||||||
| Formula | C32H33N3O7S | ||||||||||||
| Molar Mass | 603.69 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Clark P, et al. MF498 [N-{[4-(5,9-Diethoxy-6-oxo-6,8-dihydro-7H-pyrrolo[3,4-g]quinolin-7-yl)-3-methylbenzyl]sulfonyl}-2-(2-methoxyphenyl)acetamide], a selective E prostanoid receptor 4 antagonist, relieves joint inflammation and pain in rodent models of rheumatoid and osteoarthritis. J Pharmacol Exp Ther. 2008 May;325(2):425-434. [2]. Xu H, et al. The Prostaglandin E2 Receptor EP4 Promotes Vascular Neointimal Hyperplasia through Translational Control of Tenascin C via the cAPM/PKA/mTORC1/rpS6 Pathway. Cells. 2022 Aug 31;11(17):2720. |