203715

BQ-610 - Calbiochem

A highly selective ETA receptor antagonist (IC₅₀ = 20 nM) that attenuates ET-induced reduction in cardiac output.

• Synonym(e): BQ-610 - Calbiochem
• Empirische Formel (Hill-System): C₃₆H₄₇N₇O₆
• Molekulargewicht: 673.80
• UNSPSC-Code: 12352200

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥90% (HPLC)
• Form: lyophilized powder
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; desiccated (hygroscopic)
• Farbe: white
• Löslichkeit: water: 1 mg/mL
• Versandbedingung: ambient
• Lagertemp.: −20°C

Beschreibung

Allgemeine Beschreibung

A highly selective ET_A receptor antagonist (IC₅₀ = 20 nM) that attenuates ET-induced reduction in cardiac output. Also inhibits ET-1- and ET-3-induced activation of adenylate cyclase (IC₅₀ = 28.2 nM). BQ-610 is 30-fold more potent than BQ-123 (Cat. No. 05-23-3831) in porcine aortic smooth muscle membrane assay.

A highly selective endothelin A (ET_A) receptor antagonist (IC₅₀ = 20 nM) that attenuates ET-induced reduction in cardiac output. Inhibits ET-1 induced mitogenesis in airway smooth muscle cells in a concentration-dependent manner (IC₅₀ = 20 nM). Also inhibits ET-1 and ET-3 induced activation of adenylate cyclase (IC₅₀ = 28.2 nM). Has been shown to prevent endothelin-induced vasoconstriction. BQ-610 is 30-fold more potent than BQ-123 (Cat. No. 05-23-3831) in a porcine aortic smooth muscle assay.

Biochem./physiol. Wirkung

Cell permeable: no

Primary Target
ETA receptor antagonist

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 20 nM as ETA receptor antagonist that attenuates ET-induced reduction in cardiac output

Warnhinweis

Toxicity: Standard Handling (A)

Sequenz

Homopiperidinyl-CO-Leu-D-Trp(CHO)-D-Trp-ONH4

Physikalische Form

Supplied as an ammonium salt.

Rekonstituierung

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Sonstige Hinweise

Beyer, M.E., et al. 1999. Hypertension33, 145.
Carratu, P., et al. 1997. Am. J. Physiol.272, L1021.
Illing, B., et al. 1996. J. Cardiovasc. Pharmacol.27, 487.
Han, H., et al. 1995. J. Mol. Cell. Cardiol.27, 761.
Ishikawa, K., et al. 1992. in Peptides, Schneider and Eberle, eds. (ESCOM), p. 685.

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