BQ-610A highly selective ETA receptor antagonist

BQ-610 (CAS 141595-53-1)

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Synonym: Hexahydroazepinocarbonyl-leucyl-tryptophyl(cho)-tryptophan
Application: A highly selective ETA receptor antagonist
CAS Number: 141595-53-1
Purity: ≥90%
Molecular Weight: 656.7
Molecular Formula: C36H44N6O6
* Refer to Certificate of Analysis for lot specific data (including water content).
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BQ-610 is a highly selective ETAR (ETA receptor) antagonist (IC50= 20 nM) which attenuates ET-induced reduction in cardiac output. It 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, in porcine aortic smooth muscle membrane assay.


References

1. Han, H., et al., 1995. Endothelin-1 contributes to ischemia/reperfusion injury in isolated rat heart-attenuation of ischemic injury by the endothelin-1 antagonists BQ123 and BQ610. Journal of molecular and cellular cardiology. 27(2): 761-6. PMID: 7776381
2. Illing, B., et al., 1996. Protective effect of the specific endothelin-1 antagonist BQ610 on mechanical function and energy metabolism during ischemia/reperfusion injury in isolated perfused rat hearts. Journal of cardiovascular pharmacology. 27(4): 487-94. PMID: 8847864
3. Carratu, P., et al., 1997. ET-1 induces mitogenesis in ovine airway smooth muscle cells via ETA and ETB receptors. The American journal of physiology. 272(5 Pt 1): L1021-4. PMID: 9176269
4. Beyer, M E., et al., 1999. Inotropic effects of endothelin-1: interaction with molsidomine and with BQ 610. Hypertension. 33(1): 145-52. PMID: 9931095

Appearance :
Powder
Physical State :
Solid
Sequence :
Homopiperidinyl-CO-Leu-D-Trp(CHO)-D-Trp-ONH4
Solubility :
Soluble in water (1 mg/ml).
Storage :
Store at -20° C
Density :
1.34 g/cm3 (Predicted)
Refractive Index :
n20D 1.66 (Predicted)
IC50 :
ETAR : IC50 = 20 nM; ET-1 induced mitogenesis : IC50 = 20 nM (airway smooth muscle cells ); ET-1 and ET-3 induced activation of adenylate cyclase: IC50 = 28.2 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
123905
MDL Number :
MFCD00270700
SMILES :
CC(C)C[C@@H](C(=O)N[C@H](CC1=CN(C2=CC=CC=C21)C=O)C(=O)N[C@H](CC3=CNC4=CC=CC=C43)C(=O)O)NC(=O)N5CCCCCC5

Download SDS (MSDS)

Certificate of Analysis

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