203715

BQ-610 - Calbiochem

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

• Synonim(y): BQ-610 - Calbiochem
• Wzór empiryczny (zapis Hilla): C₃₆H₄₇N₇O₆
• Masa cząsteczkowa: 673.80
• Kod UNSPSC: 12352200

Właściwości

• Poziom jakości: 100
• Próba: ≥90% (HPLC)
• Postać: lyophilized powder
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; desiccated (hygroscopic)
• kolor: white
• rozpuszczalność: water: 1 mg/mL
• Warunki transportu: ambient
• temp. przechowywania: −20°C

Opis

Opis ogólny

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.

Działania biochem./fizjol.

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

Ostrzeżenie

Toxicity: Standard Handling (A)

Sekwencja

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

Postać fizyczna

Supplied as an ammonium salt.

Rekonstytucja

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

Inne uwagi

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.

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable