203715

BQ-610 - Calbiochem

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

• Sinonimo/i: BQ-610 - Calbiochem
• Formula empirica (notazione di Hill): C₃₆H₄₇N₇O₆
• Peso molecolare: 673.80
• Codice UNSPSC: 12352200

Proprietà

• Livello qualitativo: 100
• Saggio: ≥90% (HPLC)
• Stato: lyophilized powder
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; desiccated (hygroscopic)
• Colore: white
• Solubilità: water: 1 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: −20°C

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

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

Attenzione

Toxicity: Standard Handling (A)

Sequenza

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

Stato fisico

Supplied as an ammonium salt.

Ricostituzione

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

Altre note

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.

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable