203715

BQ-610 - Calbiochem

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

• 别名: BQ-610 - Calbiochem
• 经验公式（希尔记法）: C₃₆H₄₇N₇O₆
• 分子量: 673.80
• 分類程式碼代碼: 12352200

属性

• 品質等級: 100
• 化驗: ≥90% (HPLC)
• 形狀: lyophilized powder
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; desiccated (hygroscopic)
• 顏色: white
• 溶解度: water: 1 mg/mL
• 運輸包裝: ambient
• 儲存溫度: −20°C

说明

一般說明

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.

生化／生理作用

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

警告

Toxicity: Standard Handling (A)

序列

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

外觀

Supplied as an ammonium salt.

重構

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

其他說明

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.

法律資訊

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

安全信息

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable