PZ0326

PF-03549184

≥98% (HPLC)

• Synonym(e): N-(3′,4′-dichloro[1,1′-biphenyl]-4-yl)-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide, PF-9184
• Empirische Formel (Hill-System): C₂₁H₁₄Cl₂N₂O₄S
• CAS-Nummer: 1221971-47-6
• Molekulargewicht: 461.32
• UNSPSC-Code: 12352202
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 5 mg/mL, clear (warmed)
• Lagertemp.: 2-8°C
• InChI: 1S/C21H14Cl2N2O4S/c22-16-10-7-13(11-17(16)23)12-5-8-14(9-6-12)25-19(21(24)27)20(26)15-3-1-2-4-18(15)30(25,28)29/h1-11,26H,(H2,24,27)
• InChIKey: YGTUCAUHSJOJCQ-UHFFFAOYSA-N

Beschreibung

Biochem./physiol. Wirkung

PF-03549184 (PF-9184) is a potent inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1) with an IC₅₀ value of 16.5 nM in recombinant human mPGES-1. mPEGS-1 is the terminal enzyme that synthesizes prostaglandin E2 (PGE2) from PGH2 to PGE2 downstream of cyclooxygenase-2 (COX-2). Its expression is induced in response to pro-inflammatory mediators, similar to COX-2. Unlike the effects of COX inhibition, PF-9184 does not inhibit the production of other PGH2-derived products such as 6-keto-PGFα or PGF2α. PF-9184 inhibits PGE2 production in cell based assays with IC₅₀ ranges from 0.5 to 5 μM. IC₅₀ concentrations for rhCOX1 and rHCOX2 are 118 μM and 236 μM, respectively.

PGE2 is involved in inflammation and is one of the most abundant prostanoid.

Sicherheitshinweise

• Piktogramme: GHS07
• Signalwort: Warning
• H-Sätze: H315,H319,H335
• P-Sätze: P261 - P264 - P271 - P280 - P302 + P352 - P305 + P351 + P338
• Gefahreneinstufungen: Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
• Zielorgane: Respiratory system
• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable