All Photos(1)
Synonym(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
Empirical Formula (Hill Notation):
C18H25F3N2O4S
Recommended Products
Assay
≥98% (HPLC)
Quality Level
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
white
solubility
DMSO: 50 mg/mL
storage temp.
−20°C
General description
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 (Cmax = 100 nM; Tmax = 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 (Cmax = 100 nM; Tmax = 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.
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
C5aR
C5aR
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Moriconi, A., et al. 2014. PNAS.111, 16937.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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