559410

SB 290157

A non-peptide that acts as a selective, high affinity, competitive antagonist of the anaphylatoxin C3a receptor (IC₅₀ = 200 nM).

• Synonym(s): SB 290157, N²-[(2,2-Diphenylethoxy)acetyl]-L-arginine, TFA
• Empirical Formula (Hill Notation): C₂₂H₂₈N₄O₄ · xC₂HF₃O₂
• CAS Number: 1140525-25-2
• Molecular Weight: 412.48 (free base basis)
• UNSPSC Code: 12352202
• NACRES: NA.25

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: lyophilized
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• solubility: DMSO: 5 mg/mL
• shipped in: ambient
• storage temp.: −20°C

Description

General description

A non-peptide that acts as a selective, high affinity, competitive antagonist of the anaphylatoxin C3a receptor (IC₅₀ = 200 nM). Does not antagonize C5aR or other chemotactic G-protein-coupled receptors. Blocks 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). Also blocks C3a-mediated ATP release from Guinea pig platelets (IC₅₀ = 30 nM). Exhibits anti-inflammatory properties. Supplied as a trifluoroacetate salt.

A non-peptide with anti-inflammatory properties that acts as a selective, high affinity, competitive antagonist of the anaphylatoxin C3a receptor (C3aR; IC₅₀ = 200 nM). Does not antagonize C5aR or other chemotactic G-protein coupled receptors. Blocks 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). Also blocks C3a-mediated ATP release from guinea pig platelets (IC₅₀ = 30 nM).

Biochem/physiol Actions

Cell permeable: no

Primary Target
C3a receptor

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 200 nM against the anaphylatoxin C3a receptor; 7, 12.5, and 27.7 nM, in blocking 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

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, 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.

Other Notes

Ames, R.S., et al. 2001. J. Immunol. 166, 6341.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable