203715

BQ-610 - Calbiochem

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

• Synonym(s): BQ-610 - Calbiochem
• Empirical Formula (Hill Notation): C₃₆H₄₇N₇O₆
• Molecular Weight: 673.80
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥90% (HPLC)
• form: lyophilized powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic)
• color: white
• solubility: water: 1 mg/mL
• shipped in: ambient
• storage temp.: −20°C

Description

General description

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 Actions

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

Warning

Toxicity: Standard Handling (A)

Sequence

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

Physical form

Supplied as an ammonium salt.

Reconstitution

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

Other Notes

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.

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