Name: Carvedilol
Brand: Selleck Chemicals
SKU: S1831
Rating: 5 (5 reviews)

Carvedilol (BM-14190, SKF 105517) is a non-selective beta blocker/alpha-1 blocker, used to treat congestive heart failure (CHF) and high blood pressure.

Carvedilol Chemical Structure

CAS: 72956-09-3

Selleck's Carvedilol has been cited by 5 publications

Purity & Quality Control

Batch: Purity: 100.0%

100.0

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Related Targets	α-adrenergic receptor β-adrenergic receptor Beta-Adrenergic Receptor	Click to Expand
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Signaling Pathway

Adrenergic Receptor Signaling Pathway

Choose Selective Adrenergic Receptor Inhibitors

Cell Data

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
ScN2a-cl3 cells	Cytotoxicity assay		Cytotoxicity against mouse dividing ScN2a-cl3 cells assessed as cell viability after 5 days by calcein-AM staining-based fluorescence assay, LC50=6.1 μM	24183589
HEK293 cells	Function assay	3 mins	Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay, IC50=7.5 μM	23241029
CHO cells	Function assay		Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique, IC50=10.4713 μM	18448342
BESM cells	Cytotoxicity assay	88 h	Cytotoxicity against BESM cells after 88 hrs by HTS assay, EC50=31 μM	20547819
Click to View More Cell Line Experimental Data

Biological Activity

Description

Carvedilol (BM-14190, SKF 105517) is a non-selective beta blocker/alpha-1 blocker, used to treat congestive heart failure (CHF) and high blood pressure.

Targets

α1-adrenergic receptor ^[1]

β1-adrenergic receptor ^[1]

In vitro
In vitro	Carvedilol rapidly inhibits Fe(++)-initiated lipid peroxidation, measured as thiobarbituric acid reactive substance (TBARS), in rat brain homogenate with an IC50 of 8.1 mM. Carvedilol protects against Fe(++)-induced alpha-tocopherol depletion in rat brain homogenate with an IC50 of 17.6 mM. Carvedilol dose-dependently decreases the intensity of the DMPO-OH signal with an IC50 of 25 mM. ^[1] Carvedilol has inverse efficacy for stimulating G(s)-dependent adenylyl cyclase but stimulates phosphorylation of the receptor's cytoplasmic tail on previously documented G protein-coupled receptor kinase sites in beta2 adrenergic receptor (beta2AR)-expressing HEK-293 cells. ^[2] Carvedilol (0.1-10 mM) produces a concentration-dependent inhibition of the mitogenesis stimulated by platelet-derived growth factor, epidermal growth factor, thrombin, and serum in human cultured pulmonary artery vascular smooth muscle cells, with IC50 values ranging from 0.3 mM to 2.0 mM. Carvedilol also produces a concentration-dependent inhibition of vascular smooth muscle cell migration induced by platelet-derived growth factor, with an IC50 value of 3 mM. ^[3] Carvedilol decreases the extent of cellular vacuolization in cardiac myocytes and prevents the inhibitory effect of doxorubicin on mitochondrial respiration in both heart and liver. Carvedilol also prevents the decrease in mitochondrial Ca(2+) loading capacity and the inhibition of the respiratory complexes of heart mitochondria caused by doxorubicin. ^[4]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT06078436	Recruiting	Heart Failure With Reduced Ejection Fraction\|Cardiogenic Shock	Min-Seok Kim\|Asan Medical Center	January 2024	Not Applicable
NCT06041932	Not yet recruiting	Liver Cirrhosis	Institute of Liver and Biliary Sciences India	November 1 2023	Not Applicable
NCT06004453	Recruiting	Heart Failure	Novartis Pharmaceuticals\|Novartis	April 5 2023	--
NCT05767229	Not yet recruiting	Portal Hypertension	Institute of Liver and Biliary Sciences India	March 15 2023	Not Applicable
NCT05057572	Unknown status	Liver Cirrhosis	Institute of Liver and Biliary Sciences India	October 1 2021	Not Applicable
NCT04198259	Unknown status	Gastric Varices Bleeding\|Liver Cirrhoses	Air Force Military Medical University China	June 1 2020	Not Applicable

References

[4] Santos DL, et al. Toxicol Appl Pharmacol, 2002, 185(3), 218-227.

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Chemical Information & Solubility

Molecular Weight	406.47	Formula	C₂₄H₂₆N₂O₄
CAS No.	72956-09-3	SDF	Download Carvedilol SDF
Smiles	COC1=CC=CC=C1OCCNCC(COC2=CC=CC3=C2C4=CC=CC=C4N3)O
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 81 mg/mL ( (199.27 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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