| Bioactivity | mPGES-1-IN-2 (compound III) is a benzimidazole-based mPGES-1 inhibitor that also inhibits adipophysin PGD synthase (I-PGDS) (5 μM, IR=60 %). mPGES-1-IN-2 reduces PGE2 production and tends to reduce levels of other prostaglandins. mPGES-1-IN-2 effectively inhibits acute inflammation in an air sac model stimulated by Carrageenan (HY-125474) in mice[1]. | ||||||||||||
| Target | IC50: 0.9 μM (recombinant human mPGES-1), 0.09 μM (recombinant rat mPGES-1); lipocalin-type PGD synthase (I-PGDS) | ||||||||||||
| Invitro | mPGES-1-IN-2 (compound III) (0.64-80 μM; 24 h) 可减少 A549 细胞、小鼠巨噬细胞和血液中，LPS (10 ng/mL) 刺激后导致的 PGE2 产生[1]。mPGES-1-IN-2 () 以浓度依赖性方式抑制 PGE2 合成，导致 PGH2 分流至前列环素途径[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> mPGES1-IN-7 相关抗体: | ||||||||||||
| In Vivo | mPGES-1-IN-2 (compound III) (10-100 mg/kg; ip; 单剂量) 在 1% λ-Carrageenan (HY-N9470) 诱导的小鼠气囊炎症模型中，有效抑制前列腺素整体的合成情况，并减少细胞迁移[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: | ||||||||||||
| CAS | 1268709-57-4 | ||||||||||||
| Formula | C23H34N4O | ||||||||||||
| Molar Mass | 382.54 | ||||||||||||
| Appearance | 固体 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. Leclerc P, et al. Characterization of a human and murine mPGES-1 inhibitor and comparison to mPGES-1 genetic deletion in mouse models of inflammation. Prostaglandins Other Lipid Mediat. 2013 Dec;107:26-34. |
mPGES1-IN-7
CAS: 1268709-57-4 F: C23H34N4O W: 382.54
mPGES-1-IN-2 (compound III) is a benzimidazole-based mPGES-1 inhibitor that also inhibits adipophysin PGD synthase (I-PG
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