SB290157 trifluoroacetate

CAS No. 1140525-25-2

SB290157 trifluoroacetate ( —— )

Catalog No. M22442 CAS No. 1140525-25-2

SB290157 trifluoroacetate is a potent and selective antagonist of C3a receptor(IC50 of 200 nM). SB 290157 is a competitive antagonist of 125I-C3a radioligand binding to rat basophilic leukemia-2H3 cells expressing the human C3aR (RBL-C3aR, IC50 of 200 nM).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    SB290157 trifluoroacetate
  • Note
    Research use only, not for human use.
  • Brief Description
    SB290157 trifluoroacetate is a potent and selective antagonist of C3a receptor(IC50 of 200 nM). SB 290157 is a competitive antagonist of 125I-C3a radioligand binding to rat basophilic leukemia-2H3 cells expressing the human C3aR (RBL-C3aR, IC50 of 200 nM).
  • Description
    SB290157 trifluoroacetate is a potent and selective antagonist of C3a receptor(IC50 of 200 nM). SB 290157 is a competitive antagonist of 125I-C3a radioligand binding to rat basophilic leukemia-2H3 cells expressing the human C3aR (RBL-C3aR, IC50 of 200 nM). SB 290157 blocks C3a-induced C3aR internalization in a concentration-dependent manner and C3a-induced Ca2+ mobilization in RBL-C3aR cells and human neutrophils (IC50s of 27.7 and 28 nM, respectively). SB 290157 is selective for the C3aR in that. SB 290157 also inhibits C3a-induced Ca2+ mobilization of RBL-2H3 cells expressing the mouse and guinea pig C3aRs. It potently inhibits C3a-mediated ATP release from guinea pig platelets and inhibits C3a-induced potentiation of the contractile response to field stimulation of perfused rat caudal artery.Neutrophil recruitment in a guinea pig LPS-induced airway neutrophilia model inhibited by SB 290157 ,SB 290157 decreases paw edema in a rat adjuvant-induced arthritis model[1]. The antagonist is able to reduce joint swelling only at 3 h, and about 50% inhibition of joint swelling is observed with the concentration of 30 mg/kg. The C3 level is significantly decreased at 3 h compared with naive mice showing complement consumption. Furthermore, the C3 activation is observed and increased corresponding to the graded concentration of anti-OVA pAb.
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    C3a
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1140525-25-2
  • Formula Weight
    526.51
  • Molecular Formula
    C24H29F3N4O6
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:125 mg/mL (237.41 mM; Need ultrasonic)
  • SMILES
    OC(=O)C(F)(F)F.NC(=N)NCCC[C@H](NC(=O)COCC(c1ccccc1)c1ccccc1)C(O)=O
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Ames RS, et al. Identification of a selective nonpeptide antagonist of the anaphylatoxin C3areceptor that demonstrates antiinflammatory activity in animal models. J Immunol. 2001 May 15;166(10):6341-8.
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