Carvedilol

Catalog No.S1831 Synonyms: BM-14190, SKF 105517

Carvedilol Chemical Structure

Molecular Weight(MW): 406.47

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

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 60 In stock
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Biological Activity

Description Carvedilol 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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
ScN2a-cl3 cells MlrCR5l1d3SxeHnjbZR6KGG|c3H5 MnO3R5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3Wg[Il3cWSrbnegV4NPOmFvY3yzJINmdGy|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDViZHH5d{BjgSClYXzj[YlvNUGPIIP0ZYlvcW6pLXLhd4VlKG[udX;y[ZNk\W6lZTDhd5NigSxiTFO1NF03NjFizszN M2rJfVI1OTh|NUi5
HEK293 cells NIrQSnpHfW6ldHnvckBie3OjeR?= M2TxWlMhdWmwcx?= MVHJcohq[mm2aX;uJI9nKGi3bXHuJG9EXDJvbXXkbYF1\WRiQWPQL{B2eHSja3Wg[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczDh[pRmeiB|IH3pcpMh[nliZnz1c5Jme2OnbnPlJIF{e2G7LDDJR|UxRTdwNTFOwG0> MmHkNlMzPDFyMkm=
CHO cells M17HS2Z2dmO2aX;uJIF{e2G7 NHG0PWlKdmirYnn0bY9vKG:oIHj1cYFvKEWURzDlfJBz\XO|ZXSgbY4hS0iRIHPlcIx{KGK7IIfoc4xmKGOnbHygdIF1[2hiY3zhcZAhfGWlaH7pdZVmNCCLQ{WwQVExNjR5MUOg{txO MXixPFQ1QDN2Mh?=
BESM cells MWHDfZRwfG:6aXPpeJkh[XO|YYm= NFKxc3Y5QCCq NWOxT2tlS3m2b4TvfIlkcXS7IHHnZYlve3RiQlXTUUBk\WyuczDh[pRmeiB6ODDodpMh[nliSGTTJIF{e2G7LDDFR|UxRTNzIN88US=> M3izU|IxPTR5OEG5

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Protocol

Solubility (25°C)

In vitro DMSO 81 mg/mL (199.27 mM)
Ethanol 4 mg/mL (9.84 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 406.47
Formula

C24H26N2O4

CAS No. 72956-09-3
Storage powder
Synonyms BM-14190, SKF 105517

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02066649 Withdrawn Portal Hypertension Related to Cirrhosis Rutgers, The State University of New Jersey February 2017 Phase 3
NCT02944201 Not yet recruiting Prostate Cancer Montefiore Medical Center|Albert Einstein College of Medicine of Yeshiva University December 2016 Phase 2
NCT02251509 Not yet recruiting Atrial Fibrillation Creighton University December 2016 Phase 4
NCT02945982 Not yet recruiting Portal Hypertension ShuGuang Hospital|Ruijin Hospital|Shanghai Zhongshan Hospital|Longhua Hospital|Shanghai Public Health Clinical Center December 2016 Phase 4
NCT02946892 Not yet recruiting Single Ventricle|Fontan University of Texas Southwestern Medical Center|American Heart Association November 2016 Phase 4
NCT02907749 Not yet recruiting Cirrhosis|Portal Hypertension Changqing Yang|Nanfang Hospital of Southern Medical University|Fudan University|Shanghai Tongji Hospital, Tongji University School of Medicine October 2016 Phase 4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID