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BQ-123 . sodium salt

CHF 140.00
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AG-CP3-0001-M0011 mgCHF 140.00
AG-CP3-0001-M0055 mgCHF 500.00
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Product Details
Synonyms Endothelin Receptor A Antagonist BQ-123; cyclo(-D-Trp-D-Asp-Pro-D-Val-Leu) . Na
Product Type Chemical
Properties
Formula

C31H42N6O7 . Na

MW 609.7 . 23.0
CAS 136655-57-7
Source/Host Chemicals Synthetic.
Purity Chemicals ≥98% (HPLC)
Appearance White solid.
Solubility Soluble in water.
InChi Key FLIKEIGEOXCRRG-DRBUQPBJSA-M
Smiles [Na+].CC(C)CC1NC(=O)[C@H](NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC([O-])=O)NC(=O)[C@@H](CC2=CNC3=C2C=CC=C3)NC1=O)C(C)C
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Handling Advice After reconstitution, prepare aliquots and store at -20°C.
Use/Stability Stable for at least 3 years after receipt when stored at -20°C.
Documents
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Product Specification Sheet
Datasheet Download PDF
Description
  • Potent and selective endothelin receptor A (ETA) antagonist [1-3].
  • Suppresses the ET-1-induced decrease of LPL activity [4].
  • Shows protective effects in ischemic acute renal failure [5].
  • Neuroprotective [6, 10].
  • Anti-hypertensive [7].
  • Inhibits ET-1 receptor binding and blocks Ca2+ mobilization, cellular contraction and MAP kinase activation [8].
  • Cardiovascular agent [9].
  • Reduces myocardial infarct size and oxidant injury [11].
  • Selected Reviews [12, 13].
Product References
  1. 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)
  2. 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)
  3. Biological profiles of highly potent novel endothelin antagonists selective for the ETA receptor: M. Ihara, et al.; Life Sci. 50, 247 (1992)
  4. 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)
  5. 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)
  6. Peptidic endothelin-1 receptor antagonist, BQ-123, and neuroprotection: G. Feuerstein, et al.; Peptides 15, 467 (1994)
  7. 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)
  8. 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)
  9. Inhibition of myocardial endothelin pathway improves longterm survival in heart failure: S. Sakai, et al.; Nature 384, 353 (1996)
  10. 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)
  11. Selective endothelin a (ETA) receptor antagonist (BQ-123) reduces both myocardial infarct size and oxidant injury: R. Ozdemir, et al.; Toxicology 219, 142 (2006)
  12. Endothelin receptor antagonists: S. Motte, et al.; Pharmacol. Ther. 110, 386 (2006) (Review)
  13. ETA-receptor antagonists or allosteric modulators?: J.G. De Mey, et al.; TIPS 32, 345 (2011) (Review)
  14. Endothelin A receptor inhibition increases nitric oxide-dependent vasodilation independent of superoxide in non-Hispanic Black young adults: C.G. Turner, et al.; J. Appl. Physiol. 134, 891 (2023)
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