SB 290157 trifluoroacetate

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Cat.No. 6860 - SB 290157 trifluoroacetate | C22H28N4O4.CF3CO2H | CAS No. 1140525-25-2
Description: Potent C3a receptor antagonist
Chemical Name: N2-[2-(2,2-Diphenylethoxy)acetyl]-L-arginine trifluoroacetate
Purity: ≥97% (HPLC)
Datasheet
Citations
Reviews
Literature (2)

Biological Activity

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.

Technical Data

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 52.65 100
ethanol 52.65 100

Preparing Stock Solutions

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.

Select a batch to recalculate based on the batch molecular weight:
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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References

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


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Citations for SB 290157 trifluoroacetate

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