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SB 290157 trifluoroacetate salt (CAS 1140525-25-2)

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Alternate Names:
N2-[(2,2-Diphenylethoxy)acetyl]-L-arginine trifluoroacetate
Application:
SB 290157 trifluoroacetate salt is a selective, high affinity, competitive antagonist of anaphylatoxin C3a receptor
CAS Number:
1140525-25-2
Purity:
≥95%
Molecular Weight:
526.50
Molecular Formula:
C22H28N4O4•CF3CO2H
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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SB 290157 trifluoroacetate salt is a non-peptide that acts as a selective, high affinity, competitive antagonist of the anaphylatoxin C3aR (C3a receptor, IC50 = 200 nM). The chemical does not antagonize C5aR or other chemotactic G-protein-coupled receptors. The compound may act to block C3a-induced internalization of C3aR in human neutrophils and C3a-induced Ca2+ mobilization in basophilic leukemia RBL-2H3 cells expressing murine, guinea pig, or human C3aR (IC50 = 7, 12.5, and 27.7 nM, respectively). SB 290157 has also been shown to block C3a-mediated ATP release from Guinea pig platelets (IC50 = 30 nM). In addition, the compound has exhibited antiinflammatory properties.


SB 290157 trifluoroacetate salt (CAS 1140525-25-2) References

  1. Identification of a selective nonpeptide antagonist of the anaphylatoxin C3a receptor that demonstrates antiinflammatory activity in animal models.  |  Ames, RS., et al. 2001. J Immunol. 166: 6341-8. PMID: 11342658
  2. Mobilization studies in mice deficient in either C3 or C3a receptor (C3aR) reveal a novel role for complement in retention of hematopoietic stem/progenitor cells in bone marrow.  |  Ratajczak, J., et al. 2004. Blood. 103: 2071-8. PMID: 14604969
  3. Complement factors C3a and C5a have distinct hemodynamic effects in the rat.  |  Proctor, LM., et al. 2009. Int Immunopharmacol. 9: 800-6. PMID: 19285573
  4. Effect of the C3a-receptor antagonist SB 290157 on anti-OVA polyclonal antibody-induced arthritis.  |  Hutamekalin, P., et al. 2010. J Pharmacol Sci. 112: 56-63. PMID: 20051658
  5. Role of complement 3a in the synthetic phenotype and angiotensin II-production in vascular smooth muscle cells from spontaneously hypertensive rats.  |  Han, Y., et al. 2012. Am J Hypertens. 25: 284-9. PMID: 22089112
  6. Role of complement 3a in the growth of mesangial cells from stroke-prone spontaneously hypertensive rats.  |  Ikeda, K., et al. 2014. Clin Exp Hypertens. 36: 58-63. PMID: 23713944
  7. Complement C3a binding to its receptor as a negative modulator of Th2 response in liver injury in trichloroethylene-sensitized mice.  |  Wang, F., et al. 2014. Toxicol Lett. 229: 229-39. PMID: 24974766
  8. Derivation of ligands for the complement C3a receptor from the C-terminus of C5a.  |  Halai, R., et al. 2014. Eur J Pharmacol. 745: 176-81. PMID: 25446428
  9. Acute physiological changes caused by complement activators and amphotericin B-containing liposomes in mice.  |  Őrfi, E., et al. 2019. Int J Nanomedicine. 14: 1563-1573. PMID: 30880965
  10. Intracortical Administration of the Complement C3 Receptor Antagonist Trifluoroacetate Modulates Microglia Reaction after Brain Injury.  |  Surugiu, R., et al. 2019. Neural Plast. 2019: 1071036. PMID: 31814819
  11. C3a receptor antagonist therapy is protective with or without thrombolysis in murine thromboembolic stroke.  |  Ahmad, S., et al. 2020. Br J Pharmacol. 177: 2466-2477. PMID: 31975437
  12. The 'C3aR Antagonist' SB290157 is a Partial C5aR2 Agonist.  |  Li, XX., et al. 2020. Front Pharmacol. 11: 591398. PMID: 33551801
  13. C3/C3aR inhibition alleviates GMH-IVH-induced hydrocephalus by preventing microglia-astrocyte interactions in neonatal rats.  |  Tang, J., et al. 2022. Neuropharmacology. 205: 108927. PMID: 34921829
  14. The role of reactive astrocytes in neurotoxicity induced by ultrafine particulate matter.  |  Li, B., et al. 2023. Sci Total Environ. 867: 161416. PMID: 36621481
  15. Macrophages promote heat stress nephropathy in mice via the C3a-C3aR-TNF pathway.  |  Yang, Y., et al. 2023. Immunobiology. 228: 152337. PMID: 36689826

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

SB 290157 trifluoroacetate salt, 10 mg

sc-222291
10 mg
$166.00

SB 290157 trifluoroacetate salt, 50 mg

sc-222291A
50 mg
$624.00

SB 290157 trifluoroacetate salt, 100 mg

sc-222291B
100 mg
$1040.00

Solubility in DMSO?

Asked by: chemicalsmg
Thank you for your question. SB 290157 trifluoroacetate salt: sc-222291 is soluble in DMSO at 5 mg/ml.
Answered by: Chemical Support 3
Date published: 2017-04-07

How should this be stored after reconstitution?

Asked by: chemicalsmg
Thank you for your question. Following reconstitution, SB 290157 trifluoroacetate salt: sc-222291, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. Do not reuse solutions diluted in physiological buffers.
Answered by: Chemical Support 3
Date published: 2017-04-07
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Rated 5 out of 5 by from WangWang, F. et al. (PubMed 24974766) used SB 290157 trifluoroacetate salt, a selective, high affinity, competitive antagonist of C3a receptor, to demonstrate that blocking of C3a binding to C3aR reduces IL4, shifts IFN- and IL-4 balance, and aggravates TCE-sensitization induced liver damage. -SCBT Publication Review
Date published: 2015-04-05
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SB 290157 trifluoroacetate salt is rated 5.0 out of 5 by 1.
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