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- Technische Daten
- Im Angebot als 1 mg (sc-296707) und 5 mg (sc-296707A) sizes
- CAS Nummer: 916482-17-2
- Molekulargewicht: 408.0
- Summenformel: C20H26ClN3O2S
- Physisches Aussehen: A solution in methyl acetate
- Beschreibung
- Microsomal prostaglandin E2 synthase-1 (mPGES-1), with cyclooxygenase-2 (COX-2), synthesizes PGE2, which is directly involved in signaling during inflammation, fever, and pain. 5-Lipoxygenase (5-LO) initiates the synthesis of leukotrienes (LTs), which are pro-inflammatory mediators. YS121 is a dual inhibitor of mPGES-1 (IC50 = 3.9 μM) and 5-LO (IC50 = 4. μM). It effectively inhibits PGE2 and LT synthesis in both cell free and intact cell assays. Moreover, YS121 (1. mg/kg, intraperitoneal) reduced pleural levels of PGE2 and LTB4 while blocking exudate formation and leukocyte infiltration in carrageenan-induced rat pleurisy. YS121 has minor effects on COX-1 and COX-2, inhibiting these enzymes 24.8% and 38%, respectively, at 10 μM
- LAGERUNG:
- Ausschließlich für Forschungszwecke (in-vitro, laboratory research use only)
- Weitere Referenznummern
- Literaturhinweise
- 1 Koeberle, A., Zettl, H., Greiner, C., et al. Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase. J Med Chem 51 8068-8076 (2008).
2 Werz, O., Greiner, C., Koeberle, A., et al. Novel and potent inhibitors of 5-lipoxygenase product synthesis based on the structures of pirinixic acid. J Med Chem 51 5449-5453 (2008).
3 Koeberle, A., Rossi, A., Zettl, H., et al. The molecular pharmacology and in vivo activity of 2-(4-chloro-6-(2,3-dimethylphenylamino)pyrimidin-2-ylthio)octanoic acid (YS121), a dual inhibitor of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase. J Pharmacol Exp Ther 332 840-848 (2010).
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Lieferzeit: 3-5 Werktage
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YS121
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