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Submit ReviewSB 290157 trifluoroacetate
Description: Potent C3a receptor antagonist
Chemical Name: N2-[2-(2,2-Diphenylethoxy)acetyl]-L-arginine trifluoroacetate
Purity: ≥97% (HPLC)
Biological Activity for SB 290157 trifluoroacetate
SB 290157 trifluoroacetate is a potent C3a receptor antagonist (IC50 values are 27 - 30 nM for C3a-induced Ca2+ mobilization in vitro and ex vivo). Inhibits C3a-induced chemotaxis in human mast cell line. Also inhibits tau hyperphosphorylation in vitro. Displays anti-inflammatory effects in animal models of airway inflammation and arthritis. Also inhibits glucose-induced insulin secretion and ATP production from ex vivo human and mouse pancreatic islets. Also exhibits C3a receptor agonist activity.
Technical Data for SB 290157 trifluoroacetate
| M. Wt | 526.51 |
| Formula | C22H28N4O4.CF3CO2H |
| Storage | Desiccate at RT |
| Purity | ≥97% (HPLC) |
| CAS Number | 1140525-25-2 |
| PubChem ID | 16760645 |
| InChI Key | ZJRMPPVJAQWGEG-FYZYNONXSA-N |
| Smiles | NC(NCCC[C@@H](C(O)=O)NC(COCC(C1=CC=CC=C1)C2=CC=CC=C2)=O)=N.FC(F)(C(O)=O)F |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for SB 290157 trifluoroacetate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 52.65 | 100 | |
| ethanol | 52.65 | 100 |
Preparing Stock Solutions for SB 290157 trifluoroacetate
The following data is based on the product molecular weight 526.51. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.9 mL | 9.5 mL | 18.99 mL |
| 5 mM | 0.38 mL | 1.9 mL | 3.8 mL |
| 10 mM | 0.19 mL | 0.95 mL | 1.9 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.38 mL |
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Product Datasheets for SB 290157 trifluoroacetate
References for SB 290157 trifluoroacetate
References are publications that support the biological activity of the product.
Ames et al (2001) Identification of a selective nonpeptide antagonist of the anaphylatoxin C3a receptor that demonstrates antiinflammatory activity in animal models. J.Immunol. 166 6341 PMID: 11342658
Atanes et al (2018) C3aR and C5aR1 act as key regulators of human and mouse β-cell function. Cell Mol.Life Sci. 75 715 PMID: 28921001
Hu et al (2019) Complement C3a receptor antagonist attenuates tau hyperphosphorylation via glycogen synthase kinase 3β signaling pathways. Eur.J.Pharmacol. 850 135 PMID: 30771350
Mathieu et al (2005) The C3a receptor antagonist SB 290157 has agonist activity. Immunol.Lett. 100 139 PMID: 16154494
If you know of a relevant reference for SB 290157 trifluoroacetate, please let us know.
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Keywords: SB 290157 trifluoroacetate, SB 290157 trifluoroacetate supplier, SB290157, trifluoroacetate, complement, system, receptor, C3a, antagonists, antagonism, antiinflammatory, chemotaxis, Complement, 6860, Tocris Bioscience
2 Citations for SB 290157 trifluoroacetate
Citations are publications that use Tocris products. Selected citations for SB 290157 trifluoroacetate include:
Yu et al (2022) C3aR Signaling Inhibits NK-cell Infiltration into the Tumor Microenvironment in Mouse Models. Cancer Immunol Res 10 245-258 PMID: 34819308
Sarah Y et al (2020) Gut Ischemia Reperfusion Injury Induces Lung Inflammation via Mesenteric Lymph-Mediated Neutrophil Activation. Front Immunol 11 586685 PMID: 33042165
Do you know of a great paper that uses SB 290157 trifluoroacetate from Tocris? Please let us know.
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