BQ-123 sodium salt (Endothelin Receptor A Antagonist BQ-123, cyclo(-D-Trp-D-Asp-Pro-D-Val-Leu) . Na)
|Biochemicals||Storage: 4°C/-20°CShipping: Blue Ice|
Potent and selective endothelin receptor A (ETA) antagonist. Suppresses the ET-1-induced decrease of LPL activity. Shows protective effects in ischemic acute renal failure. Neuroprotective. Anti-hypertensive. Inhibits ET-1 receptor binding and blocks Ca2+ mobilization, cellular contraction and MAP kinase activation. Cardiovascular agent. Reduces myocardial infarct size and oxidant injury.
Storage and Stability:
Short-term Storage: +4°C
Long-term Storage: -20°C
Stable for at least 3 years after receipt when stored at -20°C.
C31H42N6O7 . Na
Purity: >98% (HPLC)
Important Note: This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
In vitro biological profile of a highly potent novel endothelin (ET) antagonist BQ-123 selective for the ETA receptor: M. Ihara, et al.; J. Cardiovasc. Pharmacol. 20, S11 (1992)
BQ-123, cyclo(-D-Trp-D-Asp-Pro-D-Val-Leu), is a non-competitive antagonist of the actions of endothelin-1 in SK-N-MC human neuroblastoma cells: C.R. Hiley, et al.; BBRC 184, 504 (1992)
Biological profiles of highly potent novel endothelin antagonists selective for the ETA receptor: M. Ihara, et al.; Life Sci. 50, 247 (1992)
Suppressive effects of the endothelin receptor (ETA) antagonist BQ-123 on ET-1-induced reduction of lipoprotein lipase activity in 3T3-L1 adipocytes: F. Ishida, et al.; Biochem. Pharmacol. 44, 1431 (1992)
Protective effect of a selective endothelin receptor antagonist, BQ-123, in ischemic acute renal failure in rats: N. Mino, et al.; Eur. J. Pharmacol. 221, 77 (1992)
Peptidic endothelin-1 receptor antagonist, BQ-123, and neuroprotection: G. Feuerstein, et al.; Peptides 15, 467 (1994)
BQ-123, a selective endothelin subtype A-receptor antagonist, lowers blood pressure in different rat models of hypertension: S.A. Douglas, et al.; J. Hypertens. 12, 561 (1994)
Inhibitory effect of BQ-123 on endothelin-1-stimulated mitogen-activated protein kinase and cell growth of rat vascular smooth muscle cells: X. Guo, et al.; Hypertens. Res. 19, 23 (1996)
Inhibition of myocardial endothelin pathway improves longterm survival in heart failure: S. Sakai, et al.; Nature 384, 353 (1996)
Similar protective effects of BQ-123 and erythropoietin on survival of neural cells and generation of neurons upon hypoxic injury: L. Danielyan, et al.; Eur. J. Cell Biol. 84, 907 (2005)
Selective endothelin a (ETA) receptor antagonist (BQ-123) reduces both myocardial infarct size and oxidant injury: R. Ozdemir, et al.; Toxicology 219, 142 (2006)
Endothelin receptor antagonists: S. Motte, et al.; Pharmacol. Ther. 110, 386 (2006) (Review)
ETA-receptor antagonists or allosteric modulators?: J.G. De Mey, et al.; TIPS 32, 345 (2011) (Review)