Carvedilol

  • CAT Number: A000894
  • CAS Number: 72956-09-3
  • Molecular Formula: C24H26N2O4
  • Molecular Weight: 406.5
  • Purity: ≥95%
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Carvedilol is a non-selective beta-adrenoceptor blocking agent (S(-) enantiomer) and as an alpha 1-adrenoceptor blocker (R(+) and S(-) enantiomers) indicated in the treatment of mild to moderate congestive heart failure (CHF). Its acts more strongly on beta-receptors than on alpha 1-receptors, reduces peripheral vascular resistance by vasodilation, and prevents reflex tachycardia (beta-blockade) so that heart rate is either unchanged or decreased.It blocks beta-1 and beta-2 adrenergic receptors as well as the alpha-1 adrenergic receptors. Carvedilol is a synthetic antihypertensive methoxyphenoxy- 2-propanol derivative with no intrinsic sympathomimetic activity. Carvedilol also reduces renin release through beta-blockade.

Catalog Number A000894
CAS Number 72956-09-3
Molecular Formula

C24H26N2O4

Purity 95%
Target Adrenergic Receptor
Solubility >20.3mg/mL in DMSO
Storage -20°C
InChI 1S/C24H26N2O4/c1-28-21-10-4-5-11-22(21)29-14-13-25-15-17(27)16-30-23-12-6-9-20-24(23)18-7-2-3-8-19(18)26-20/h2-12,17,25-27H,13-16H2,1H3
InChIKey OGHNVEJMJSYVRP-UHFFFAOYSA-N
SMILES COC1=CC=CC=C1OCCNCC(COC2=CC=CC3=C2C4=CC=CC=C4N3)O
Reference

1: Zawadzka K, Bernat P, Felczak A, Różalska S, Lisowska K. Antibacterial
activity of high concentrations of carvedilol against gram-positive and
gram-negative bacteria. Int J Antimicrob Agents. 2017 Dec 22. pii:
S0924-8579(17)30448-X. doi: 10.1016/j.ijantimicag.2017.12.014. [Epub ahead of
print] PubMed PMID: 29277530.

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2: Gao P, Yang B, Yu HY, Meng RR, Si JY. Carvedilol alleviates the biliary
cirrhosis through inhibiting the endoplasmic reticulum stress. Eur Rev Med
Pharmacol Sci. 2017 Dec;21(24):5813-5820. doi: 10.26355/eurrev_201712_14029.
PubMed PMID: 29272018.
<br>

3: Ibrahim TM, Abdallah MH, El-Megrab NA, El-Nahas HM. Upgrading of dissolution
and anti-hypertensive effect of Carvedilol via two combined approaches:
self-emulsification and liquisolid techniques. Drug Dev Ind Pharm. 2017 Dec
28:1-13. doi: 10.1080/03639045.2017.1417421. [Epub ahead of print] PubMed PMID:
29254384.
<br>

4: Maharaj S, Seegobin K, Perez-Downes J, Bajric B, Chang S, Reddy P. Severe
carvedilol toxicity without overdose – caution in cirrhosis. Clin Hypertens. 2017
Nov 30;23:25. doi: 10.1186/s40885-017-0083-z. eCollection 2017. PubMed PMID:
29214053; PubMed Central PMCID: PMC5709975.
<br>

5: Roberts MA, Darssan D, Badve SV, Carroll RP, Fahim MA, Haluska BA, Hawley CM,
Isbel NM, Marshall MR, Pascoe EM, Pedagogos E, Pilmore HL, Snelling P, Stanton T,
Tan KS, Tonkin AM, Vergara LA, Ierino FL. Carvedilol and Cardiac Biomarkers in
Dialysis Patients: Secondary Analysis of a Randomized Controlled Trial. Kidney
Blood Press Res. 2017 Dec 4;42(6):1033-1044. doi: 10.1159/000485589. [Epub ahead
of print] PubMed PMID: 29197871.

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6: Abd ElRahim AY, Fouad R, Khairy M, Elsharkawy A, Fathalah W, Khatamish H,
Khorshid O, Moussa M, Seyam M. Efficacy of carvedilol versus propranolol versus
variceal band ligation for primary prevention of variceal bleeding. Hepatol Int.
2017 Nov 28. doi: 10.1007/s12072-017-9835-9. [Epub ahead of print] PubMed PMID:
29185106.
<br>

7: Y-Hassan S, Tornvall P. Reply to: metoprolol, or propranolol, or carvedilol,
or labetalol, for patients with takotsubo syndrome? Clin Auton Res. 2017 Nov 27.
doi: 10.1007/s10286-017-0483-x. [Epub ahead of print] PubMed PMID: 29181766.
<br>

8: Wang J, Hanada K, Staus DP, Makara MA, Dahal GR, Chen Q, Ahles A, Engelhardt
S, Rockman HA. Gα(i) is required for carvedilol-induced β(1) adrenergic receptor
β-arrestin biased signaling. Nat Commun. 2017 Nov 22;8(1):1706. doi:
10.1038/s41467-017-01855-z. PubMed PMID: 29167435; PubMed Central PMCID:
PMC5700200.
<br>

9: Yi R, Xiangyu G, Min S. The expression of transforming growth factor-β1 in
myocardial tissue and concentration of serum B-type natriuretic peptide in
myocardial remodeling of Sprague-Dawley rats treated with carvedilol. Eur Rev Med
Pharmacol Sci. 2017 Nov;21(21):4975-4982. PubMed PMID: 29164560.

<br>
10: Guzeloglu M, Ertuna E, Arun MZ, Reel B. Effects of carvedilol on vascular
reactivity in human left internal mammary artery. Eur Rev Med Pharmacol Sci. 2017
Nov;21(21):4983-4988. PubMed PMID: 29164559.

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