PF-9184
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- CAS-Nr.
- 1221971-47-6
- Englisch Name:
- PF-9184
- Synonyma:
- PF-9184;PF-03549184;PF9184,PF 9184;N-[3',4'-Dichloro(1,1'-biphenyl)-yl]-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide;2H-1,2-Benzothiazine-3-carboxamide, N-(3',4'-dichloro[1,1'-biphenyl]-4-yl)-4-hydroxy-, 1,1-dioxide;N-(3',4'-dichloro-[1,1'-biphenyl]-4-yl)-4-hydroxy-2H-benzo[e][1,2]thiazine-3-carboxamide 1,1-dioxide
- CBNumber:
- CB43067570
- Summenformel:
- C21H14Cl2N2O4S
- Molgewicht:
- 461.32
- MOL-Datei:
- 1221971-47-6.mol
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PF-9184 Eigenschaften
- Schmelzpunkt:
- 285.5-289.3 °C
- Dichte
- 1.574±0.06 g/cm3(Predicted)
- storage temp.
- 2-8°C
- L?slichkeit
- ≤15mg/ml in DMSO;20mg/ml in dimethyl formamide
- pka
- 4.50±1.00(Predicted)
- Aggregatzustand
- powder
- Farbe
- white to beige
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
PF-9184 Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product prostaglandin H
2 (PGH
2; ) into the biologically active PGE
2 . Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1β, and TNF-α. PF-9184 is a potent inhibitor of mPGES-1 (IC
50 = 16.5 nM for recombinant human enzyme). It displays at least 6,500-fold selectivity for mPGES-1 over COX-1 and COX-2. PF-9184 blocks the synthesis of PGE
2 in LPS-treated human whole blood and in IL-1β-stimulated fibroblasts (IC
50s = 0.4-5 μM).
Verwenden
PF 9184 is a?microsomal prostaglandin E?synthase-1(mPGES-1) inhibitor. mPGES-1is an enzyme induced during the inflammatory response and it is an attractive target for developing anti-inflammatory drugs.
Enzyminhibitor
This potent mPGES-1 inhibitor (FW = 461.32 g/mol; CAS 1221971-47-6; Solubility: 100 mM in DMSO), also named N-[3',4'-dichloro(1,1'- biphenyl)yl]-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide), targets human and rat microsomal prostaglandin E synthase 1, with respective IC50 values of 16.5 nM and 1.08 μM, exhibiting >6500x selectivity toward mPGES-1 versus COX1 and COX2. PF-9184 inhibits IL- 1β-induced PGE2 synthesis in vitro. In inflammation and clinically relevant biological systems, mPGES-1 expression, like COX-2 expression is induced in cell context- and time-dependent manner, a behavior that is fully consistent with the kinetics of PGE2 synthesis
PF-9184 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
PF-9184 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 30)Lieferanten
- PF-9184
- N-[3',4'-Dichloro(1,1'-biphenyl)-yl]-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide
- PF-03549184
- 2H-1,2-Benzothiazine-3-carboxamide, N-(3',4'-dichloro[1,1'-biphenyl]-4-yl)-4-hydroxy-, 1,1-dioxide
- PF9184,PF 9184
- N-(3',4'-dichloro-[1,1'-biphenyl]-4-yl)-4-hydroxy-2H-benzo[e][1,2]thiazine-3-carboxamide 1,1-dioxide
- 1221971-47-6
