PZ0326

PF-03549184

≥98% (HPLC)

• 別名: N-(3′,4′-dichloro[1,1′-biphenyl]-4-yl)-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide, PF-9184
• 実験式（ヒル表記法）: C₂₁H₁₄Cl₂N₂O₄S
• CAS番号: 1221971-47-6
• 分子量: 461.32
• UNSPSCコード: 12352202
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• 形状: powder
• 色: white to beige
• 溶解性: DMSO: 5 mg/mL, clear (warmed)
• 保管温度: 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)
• InChI Key: YGTUCAUHSJOJCQ-UHFFFAOYSA-N

詳細

生物化学的／生理学的作用

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.

安全性情報

• ピクトグラム: GHS07
• シグナルワード: Warning
• 危険有害性情報: H315,H319,H335
• 注意書き: P261 - P264 - P271 - P280 - P302 + P352 - P305 + P351 + P338
• 危険有害性の分類: Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
• ターゲットの組織: Respiratory system
• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable