SB 290157 (trifluoroacetate salt)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
Reference:
[1] R. S. Ames, D. Lee, J. J. Foley, et al. Identification of a selective nonpeptide antagonist of the anaphylatoxin C3a receptor that demonstrates antiinflammatory activity in animal models. Journal of Immunology 166(10), 6341-6348 (2001).
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 526.5 |
Cas No. | 1140525-25-2 |
Formula | C22H28N4O4·CF3COOH |
Solubility | ≤30mg/ml in ethanol;20mg/ml in DMSO;25mg/ml in dimethyl formamide |
Chemical Name | N2-[2-(2,2-diphenylethoxy)acetyl]-L-arginine, 2,2,2-trifluoroacetate |
SDF | Download SDF |
Canonical SMILES | O=C(N[C@H](C(O)=O)CCCNC(N)=N)COCC(C1=CC=CC=C1)C2=CC=CC=C2.FC(F)(C(O)=O)F |
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