PZ0184

PF-04457845

≥98% (HPLC)

• 別名: N-(3-pyridazinyl)-4-(3-[5-trifluoromethyl-2-pyridinyloxy]benzylidene)piperidine-1-carboxamide, N-3-Pyridazinyl-4-[[3-[[5-(trifluoromethyl)-2-pyridinyl]oxy]phenyl]methylene]-1-piperidinecarboxamide, PF-4457845
• 実験式（ヒル表記法）: C₂₃H₂₀F₃N₅O₂
• CAS番号: 1020315-31-4
• 分子量: 455.43
• MDL番号: MFCD18782721
• UNSPSCコード: 51111800
• PubChem Substance ID: 329823758
• 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: 20 mg/mL
• 保管温度: room temp
• SMILES記法: O=C(NC1=NN=CC=C1)N(CC2)CCC2=CC3=CC=CC(OC4=NC=C(C(F)(F)F)C=C4)=C3
• InChI: 1S/C23H20F3N5O2/c24-23(25,26)18-6-7-21(27-15-18)33-19-4-1-3-17(14-19)13-16-8-11-31(12-9-16)22(32)29-20-5-2-10-28-30-20/h1-7,10,13-15H,8-9,11-12H2,(H,29,30,32)
• InChI Key: BATCTBJIJJEPHM-UHFFFAOYSA-N

詳細

生物化学的／生理学的作用

PF-04457845 is a potent, orally active, irreversible inhibitor of fatty acid amide hydrolase (FAAH), the principle enzyme involved in the degradation of the endocannabinoid anandamide. PF-04457845 is a covalent inhibitor that carbamylates FAAH′s serine nucleophile. It was shown to be both potent and selective against other serine hydrolases. It has an IC50 value of 7.2 nM for human FAAH. The endocannabinoid system is a target for therapeutic pain relief. In a rat model of inflammatory pain, PF-04457845 produced significant reduction of inflammatory pain with efficacy comparable to that of naproxen at 10 mg/kg.

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable