Home Neuronal Signaling Adrenergic Receptor antagonist Carvedilol For research use only.

Carvedilol

Synonyms: BM-14190, SKF 105517

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

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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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation 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
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

Chemical lnformation & 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)

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


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In vivo
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