SB 290157 (trifluoroacetate salt)

• CAT Number: I009332
• CAS Number: 1140525-25-2(SB 290157 trifluoroacetate salt), 259218-28-5 (SB 290157).
• Molecular Formula: C24H29F3N4O6
• Molecular Weight: 526.51
• Purity: ≥95%
• Synonyms: SB 290157 (trifluoroacetate salt); SB 290157; SB-290157; SB290157.;N2-[2-(2,2-diphenylethoxy)acetyl]-L-arginine, 2,2,2-trifluoroacetate
• Target: Complement System
• Solubility: Soluble in DMSO
• Storage: 0 - 4 °C for short term, or -20 °C for long term
• IC50: 200 nM
• InChI: InChI=1S/C22H28N4O4.C2HF3O2/c23-22(24)25-13-7-12-19(21(28)29)26-20(27)15-30-14-18(16-8-3-1-4-9-16)17-10-5-2-6-11-17;3-2(4,5)1(6)7/h1-6,8-11,18-19H,7,12-15H2,(H,26,27)(H,28,29)(H4,23,24,25);(H,6,7)/t19-;/m0./s1
• InChIKey: ZJRMPPVJAQWGEG-FYZYNONXSA-N
• SMILES: N=C(N)NCCC[C@@H](C(O)=O)NC(COCC(C1=CC=CC=C1)C2=CC=CC=C2)=O.O=C(O)C(F)(F)F

SB290157 (trifluoroacetate salt) is a selective antagonist of complement anaphylatoxin C3a receptor, a 74 amino acid proinflammatory peptide that is a potent chemotaxin for eosinophils, macrophages and mast cells. SB290157 is selective for C3aR over C5aR or other chemotactic GPCRs with an IC50 of 200 nM. It effectively blocks C3aR in humans, rat, guinea pig, and mouse. SB290157 was found to inhibit diet-induced obesity, and metabolic dysfunction.

Reference

1. Ames, R.S.,Li, Y.,Sarau, H.M., et al. Molecular cloning and characterization of the human anaphylatoxin C3a receptor. The Journal of Biological Chemisty 271(34), 20231-20234 (1996).2. Ames, R.S.,Lee, D.,Foley, J.J., 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).