BQ-123 - CAS 136553-81-6
Catalog number:
136553-81-6
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C31H42N6O7
Molecular Weight:
610.7
COA:
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Targets:
Endothelin A receptor
Description:
BQ-123 is a selective endothelin A receptor (ETA) antagonist with IC50 of 7.3 nM. Phase 2.
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Purity:
98%
Appearance:
Solid powder
Synonyms:
BQ123
Solubility:
DMSO,100mg/mLwarmed(163.74mM);Ethanol,15mg/mLwarmed(24.56mM);Water,<1mg/mL(<1mM)
Storage:
3 years -20℃powder;6 months-80℃in solvent
MSDS:
Inquire
Shelf Life:
2 years if stored properly
Canonical SMILES:
O=C([C@H]1N(C([C@H](CC(O)=O)NC([C@H](CC2=CNC3=CC=CC=C23)NC4=O)=O)=O)CCC1)N[C@@H](C(N[C@H]4CC(C)C)=O)C(C)C
1.Developmental conversion of inotropism by endothelin I and angiotensin II from positive to negative in mice.
Sekine T1, Kusano H, Nishimaru K, Tanaka Y, Tanaka H, Shigenobu K. Eur J Pharmacol. 1999 Jun 25;374(3):411-5.
Inotropic effects on isolated neonatal and adult mouse myocardium of endothelin I and angiotensin II were examined. Endothelin I produced a sustained positive inotropic response in the neonate but a sustained negative response in the adult. Both were concentration-dependent and were inhibited by the endothelin ETA receptor antagonist, BQ-123 (Cyclo(D-a-aspartyl-L-prolyl-D-valyl-L-leucyl-D-tryptophyl)). Angiotensin II produced a sustained positive inotropic response in the neonate while a sustained negative response in the adult. Both were concentration-dependent and were inhibited by the angiotensin AT1 receptor antagonist, YM358 (2,7-diethyl-5-((2'-(1 H-tetrazol-5-yl)biphenyl-4-yl)methyl-5H-pyrazolo(1,5-b)(1,2,4)tria zole potassium salt monohydrate). These results indicate that inotropic responses of the mouse heart to cardioactive peptides are unique among experimental animal species and may be reversed during development.
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CAS 136553-81-6 BQ-123

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