SB290157 trifluoroacetate

SKU: orb1309121

Description

SB290157 trifluoroacetate is a selective C3a receptor antagonist with an IC50 of 200 nM. This compound is a valuable research tool for investigating the role of the C3a anaphylatoxin receptor in complement-mediated inflammatory processes, both in vitro and in vivo.

Research Area

Immunology & Inflammation

Key Properties

• CAS Number: 1140525-25-2
• MW: 526.51
• Purity: 99.89% (May vary between batches)
• Formula: C₂₄H₂₉F₃N₄O₆
• SMILES: OC(=O)C(F)(F)F.NC(=N)NCCC[C@H](NC(=O)COCC(c1ccccc1)c1ccccc1)C(O)=O
• Target: Complement System
• Solubility: DMSO:125 mg/mL (237.41 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (7.6 mM)

Bioactivity

• Target IC50:
  C3a:200 nM
• In Vivo:
  SB 290157 effectively inhibits neutrophil recruitment in a guinea pig model of LPS-induced airway neutrophilia and reduces paw edema in a rat model of adjuvant-induced arthritis. This antagonist demonstrates a capacity to decrease joint swelling, achieving approximately 50% inhibition at a concentration of 30 mg/kg, but only at the 3-hour mark. Additionally, it significantly lowers C3 levels at 3 hours post-administration, indicating complement consumption compared to naive mice. An increase in C3 activation correlates with the graded concentration of anti-OVA pAb, further showcasing its biological activity (1, 2).
• In Vitro:
  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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

C3a, ComplementSystem, Complement System, Inhibitor, inhibit, SB 290157, SB 290157 Trifluoroacetate, SB290157, SB-290157, SB290157 Trifluoroacetate, SB290157 trifluoroacetate, SB-290157 trifluoroacetate, SB-290157 Trifluoroacetate

Compound Identifiers

PubChem CID

16760645