BQ-123
Appearance
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Names | |
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IUPAC name
2-[(3R,6R,9S,12R,15S)-6-(1H-indol-3-ylmethyl)-9-(2-methylpropyl)-2,5,8,11,14-pentaoxo-12-propan-2-yl-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-3-yl]acetic acid
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Other names
Cyclo(D-trp-D-asp-L-pro-D-val-L-leu)
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Identifiers | |
3D model (JSmol)
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ChEMBL | |
ChemSpider | |
PubChem CID
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UNII | |
CompTox Dashboard (EPA)
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Properties | |
C31H42N6O7 | |
Molar mass | 610.712 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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BQ-123 is a cyclic peptide consisting of five amino acids. The amino acid sequence is D-tryptamine-D-aspartic acid-L-proline-D-valine-L-leucine.
BQ-123 is a selective ETA endothelin receptor antagonist.[1][2] As such, it is used as a biochemical tool in the study of endothelin receptor function. BQ-123 works as an ET-1 antagonist by reversing already established contractions to ET-1. This indicates that BQ-123 can work as an antagonist to remove ET-1 from its receptor (ETA).[3]
References
- ^ a b BQ-123 at Sigma-Aldrich
- ^ Ishikawa, Kiyofumi; Fukami, Takehiro; Nagase, Toshio; Fujita, Kagari; Hayama, Takashi; Niiyama, Kenji; Mase, Toshiaki; Ihara, Masaki; Yano, Mitsuo (1992). "Cyclic pentapeptide endothelin antagonists with high ETA selectivity. Potency- and solubility-enhancing modifications". Journal of Medicinal Chemistry. 35 (11): 1239–42. doi:10.1021/jm00089a028.
- ^ Berrazueta, José R.; Bhagat, Kiran; Vallance, Patrick; MacAllister, Raymond J. (Dec 1997). "Dose- and time-dependency of the dilator effects of the endothelin antagonist, BQ-123, in the human forearm". British Journal of Clinical Pharmacology. 44 (6): 569–571. doi:10.1046/j.1365-2125.1997.t01-1-00631.x. ISSN 0306-5251. PMC 2042881. PMID 9431833.