559410
SB 290157
A non-peptide that acts as a selective, high affinity, competitive antagonist of the anaphylatoxin C3a receptor (IC₅₀ = 200 nM).
Synonym(s):
SB 290157, N²-[(2,2-Diphenylethoxy)acetyl]-L-arginine, TFA
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About This Item
Empirical Formula (Hill Notation):
C22H28N4O4 · xC2HF3O2
CAS Number:
Molecular Weight:
412.48 (free base basis)
UNSPSC Code:
12352202
NACRES:
NA.25
Recommended Products
Quality Level
assay
≥95% (HPLC)
form
lyophilized
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
desiccated (hygroscopic)
protect from light
solubility
DMSO: 5 mg/mL
shipped in
ambient
storage temp.
−20°C
General description
A non-peptide that acts as a selective, high affinity, competitive antagonist of the anaphylatoxin C3a receptor (IC50 = 200 nM). Does not antagonize C5aR or other chemotactic G-protein-coupled receptors. Blocks C3a-induced internalization of C3aR in human neutrophils and C3a-induced Ca2+ mobilization in basophilic leukemia RBL-2H3 cells expressing murine, guinea pig, or human C3aR (IC50 = 7, 12.5, and 27.7 nM, respectively). Also blocks C3a-mediated ATP release from Guinea pig platelets (IC50 = 30 nM). Exhibits anti-inflammatory properties. Supplied as a trifluoroacetate salt.
A non-peptide with anti-inflammatory properties that acts as a selective, high affinity, competitive antagonist of the anaphylatoxin C3a receptor (C3aR; IC50 = 200 nM). Does not antagonize C5aR or other chemotactic G-protein coupled receptors. Blocks C3a-induced internalization of C3aR in human neutrophils and C3a-induced Ca2+ mobilization in basophilic leukemia RBL-2H3 cells expressing murine, guinea pig, or human C3aR (IC50 = 7, 12.5, and 27.7 nM, respectively). Also blocks C3a-mediated ATP release from guinea pig platelets (IC50 = 30 nM).
Biochem/physiol Actions
Cell permeable: no
Primary Target
C3a receptor
C3a receptor
Product does not compete with ATP.
Reversible: no
Target IC50: 200 nM against the anaphylatoxin C3a receptor; 7, 12.5, and 27.7 nM, in blocking C3a-induced internalization of C3aR in human neutrophils and C3a-induced Ca2+ mobilization in basophilic leukemia RBL-2H3 cells expressing murine, guinea pig, or human C3aR
Packaging
Packaged under inert gas
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. Do not reuse solutions diluted in physiological buffers.
Other Notes
Ames, R.S., et al. 2001. J. Immunol. 166, 6341.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
wgk_germany
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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