Name: SB 290157 (trifluoroacetate salt)
Price: 263.00 USD

- Overview
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    Background
    
    IC50: 200 nM
    SB 290157 is a C3aR antagonist.
    The anaphylatoxin C3a, a potent chemotactic peptide and inflammatory mediator, binds to and activates a G-protein-coupled receptor. Molecular cloning of the C3aR has facilitated the identification of the non-peptide C3aR antagonists.
    In vitro: SB 290157 was a competitive antagonist of 125I-C3a and binding to rat basophilic leukemia (RBL)-2H3 cells expressing the human C3aR , with an IC50 of 200 nM. SB 290157 could also block the C3a-induced C3aR internalization concentration-dependently and C3a-induced Ca21 mobilization in RBL-C3aR cells and human neutrophils. SB 290157 was founf to be selective for the C3aR in that it did not antagonize the C5aR or six other chemotactic G protein-coupled receptors. In addition, SB 290157 could also inhibit C3a induced Ca21 mobilization of RBL-2H3 cells expressing the mouse and guinea pig C3aRs [1].
    In vivo: In animal models, SB 290157 was able to inhibit neutrophil recruitment in a guinea pig LPS-induced airway neutrophilia model and decrease paw edema in a rat adjuvant-induced arthritis model [1].
    Clinical trial: So far, no clinical study has been conducted.
- Properties
  - Categories
    
    C3aR antagonist
    
    Alternative Name
    
    N2-[2-(2,2-diphenylethoxy)acetyl]-L-arginine, 2,2,2-trifluoroacetate
    
    CAS Number
    
    1140525-25-2
    
    Molecular Formula
    
    C22H28N4O4·CF3COOH
    
    Molecular Weight
    
    526.5
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    Purity ≥95.00%
    
    Solubility
    
    ≤30mg/ml in ethanol;20mg/ml in DMSO;25mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    O=C(N[[email protected]](C(O)=O)CCCNC(N)=N)COCC(C1=CC=CC=C1)C2=CC=CC=C2.FC(F)(C(O)=O)F
    
    * For Research Use Only