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.
Product Reference: |
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)
|Intended for research use only. Not for use in human, therapeutic, or diagnostic applications.|