PZ0184

PF-04457845

≥98% (HPLC)

• Synonym(s): 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
• Empirical Formula (Hill Notation): C₂₃H₂₀F₃N₅O₂
• CAS Number: 1020315-31-4
• Molecular Weight: 455.43
• MDL number: MFCD18782721
• UNSPSC Code: 51111800
• PubChem Substance ID: 329823758
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 20 mg/mL
• storage temp.: room temp
• SMILES string: 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

Description

Biochem/physiol Actions

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.

Potent irreversible FAAH inhibitor

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable