Bucindolol CAS: 71119-11-4
MF: C22H25N3O2
MW: 363.45

Bucindolol (CAS 71119-11-4)

Bucindolol | CAS 71119-11-4 is rated 5.0 out of 5 by 1.
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Alternate Names: Bucindolol is also known as DL-Bucindolol.
Application: Bucindolol is a non-selective β-AR adrenoceptor antagonist with additional α1-adrenoceptor blocking activity.
CAS Number: 71119-11-4
Purity: ≥98%
Molecular Weight: 363.45
Molecular Formula: C22H25N3O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data (including water content).
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Bucindolol is a non-selective β-adrenoceptor antagonist with additional α1-adrenoceptor blocking activity. Bucindolol acts on both β1 and β2 receptors. The Ki values are 1.61, 1.20 and 68.9 nM for β1-, β2- and α1-adrenoceptors respectively. Bucindolol also acts as a weak 5-HT2A/2B antagonist. Bucindolol displays vasodilatory and antihypertensive actions. Bucindolol can function with β-blockers in formulations to manage chronic heart failure.


References

1. Bristow, M.R., Roden, R.I., Lowes, B.D., et al.The role of third-generation beta-blocking agents in chronic heart failure. Clin. Cardiol. 21(12 Suppl 1), I3-I13 (1998).
2. Maack, C., Cremers, B., Flesch, M., et al.Different intrinsic activities of bucindolol, carvedilol and metoprolol in human failing myocardium. Br. J. Pharmacol. 130(5), 1131-1139 (2000).
3. Smart, N.A., Kwok, N., Holland, D.J., et al.Bucindolol: A pharmacogenomic perspective on its use in chronic heart failure. Clin. Med. Insights Cardiol. 5, 55-66 (2011).

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), and ethanol (50 mM).
Storage :
Store at 4° C
Melting Point :
229.56° C (Predicted)
Boiling Point :
~605.3° C at 760 mmHg (Predicted)
Density :
~1.2 g/cm3 (Predicted)
Refractive Index :
n20D 1.63 (Predicted)
IC50 :
CYP2D6: IC50 = 50 nM (human); OCT1: IC50 = 27.2 µM (human)
Ki Data :
β2-AR : Ki= 1.20 nM; β1-AR : Ki= 1.61 nM; α1A-AR : Ki= 68.9 nM
pK Values :
pKa: 13.76 (Predicted), pKb: 9.35 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
RTECS :
DI4637550
PubChem CID :
MDL Number :
MFCD00865898
SMILES :
CC(C)(CC1=CNC2=CC=CC=C21)NCC(COC3=CC=CC=C3C#N)O

Download SDS (MSDS)

Certificate of Analysis

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Bucindolol (CAS 71119-11-4)  Product Citations

See how others have used Bucindolol (CAS 71119-11-4). Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 31360296  de Lima-Seolin, BG.|Nemec-Bakk, A.|Forsyth, H.|Kirk, S.|da Rosa Araujo, AS.|Schenkel, PC.|Belló-Klein, A.|Khaper, N.| et al. 2019. Oxid Med Cell Longev. 2019: 6325424.

PMID: # 28011346  Lima-Seolin, BG.|Colombo, R.|Bonetto, JHP.|Teixeira, RB.|Donatti, LM.|Casali, KR.|Godoy, AEG.|Litvin, IE.|Schenkel, PC.|Rosa Araujo, ASD.|Belló-Klein, A.| et al. 2017. Eur J Pharmacol. 798: 57-65.

Citations 1 to 2 of 2 total
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Rated 5 out of 5 by from Maack et al Maack et al. (PubMed ID 12847069) found bucindolol was a partial agonist of human beta1-AR. -SCBT Publication Review
Date published: 2015-03-02
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