559410

SB 290157

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

• Synonym(e): SB 290157, N²-[(2,2-Diphenylethoxy)acetyl]-L-arginine, TFA
• Empirische Formel (Hill-System): C₂₂H₂₈N₄O₄ · xC₂HF₃O₂
• CAS-Nummer: 1140525-25-2
• Molekulargewicht: 412.48 (free base basis)
• UNSPSC-Code: 12352202
• NACRES: NA.25

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥95% (HPLC)
• Form: lyophilized
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; desiccated (hygroscopic); protect from light
• Löslichkeit: DMSO: 5 mg/mL
• Versandbedingung: ambient
• Lagertemp.: −20°C

Beschreibung

Allgemeine Beschreibung

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. Wirkung

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

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

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.

Sonstige Hinweise

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

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable