5.33797

C5aR Antagonist, DF2593A

• Sinônimo(s): C5aR Antagonist, DF2593A, (R)-4-(1-(4-(piperidin-1-yl)butanamido)ethyl)phenyl trifluoromethanesulfonate, C5aR Inhibitor, DF2593A, C5aR Blocker, DF2593A, C5a Receptor Antagonist, DF2593A
• Fórmula empírica (Notação de Hill): C₁₈H₂₅F₃N₂O₄S
• Número CAS: 938452-57-4
• Peso molecular: 422.46
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Ensaio: ≥98% (HPLC)
• Nível de qualidade: 100
• forma: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: white
• solubilidade: DMSO: 50 mg/mL
• temperatura de armazenamento: −20°C

Descrição

Descrição geral

An orally available, blood-brain barrier permeant piperidinylbutanamide compound that acts as a highly potent, selective, non-competitive and allosteric antagonist of C5a receptor (C5aR). Shown to effectively block C5a-induced human PMN migration (IC₅₀ = 5.0 nM) and is also effective in rat and mouse orthologs (IC₅₀ = 6.0 and 1 nM for rat and mouse, respectively). Exhibits good selectivity against a panel of GPCRs and ion channels screened and is shown to be completely inactive in a prostaglandin E2 production assay (~10 µM). Blocks C5a-induced and carrageenan-induced hyperalgesia in mice without any sedative or central opioid-like effects. Following oral administration, it is rapidly absorbed and displays favorable pharmacokinetic profile (C_max = 100 nM; T_max = 1.2 h at 1 mg/kg in mice).

An orally available, blood-brain barrier permeant piperidinylbutanamide compound that acts as a highly potent, selective, non-competitive and allosteric antagonist of C5a receptor (C5aR). Shown to effectively block C5a-induced human PMN migration (IC₅₀ = 5.0 nM) and is also effective in rat and mouse orthologs (IC₅₀ = 6.0 and 1 nM for rat and mouse, respectively). Exhibits good selectivity against a panel of GPCRs and ion channels screened and is shown to be completely inactive in a prostaglandin E2 production assay (~10 µM). Blocks C5a-induced and carrageenan-induced hyperalgesia in mice without any sedative or central opioid-like effects. Following oral administration, it is rapidly absorbed and displays favorable pharmacokinetic profile (C_max = 100 nM; T_max = 1.2 h at 1 mg/kg in mice).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
C5aR

Advertência

Toxicity: Standard Handling (A)

Reconstituição

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Outras notas

Moriconi, A., et al. 2014. PNAS.111, 16937.

Informações legais

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable