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 NGPKcoxEgXSxdH;4bYNqfHliYYPzZZk> MXXDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDkbZZq\GmwZzDTZ24z[S2lbEOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPSCmYYnzJIJ6KGOjbHPlbY4uSU1ic4ThbY5qdmdvYnHz[YQh\my3b4Lld4NmdmOnIHHzd4F6NCCOQ{WwQVYvOSEQvF2= NWjIXGVXOjRzOEO1PFk>
HEK293 cells MX\GeY5kfGmxbjDhd5NigQ>? Mln0N{BucW6| NWnRZ4hVUW6qaXLpeIlwdiCxZjDoeY1idiCRQ2SyMY1m\GmjdHXkJGFUWCtidYD0ZYtmKGW6cILld5Nm\CCrbjDISWszQTNiY3XscJMh[W[2ZYKgN{BucW6|IHL5JIZtfW:{ZYPj[Y5k\SCjc4PhfUwhUUN3ME23MlUh|ryP NYPkVY04OjN{NEGwNlk>
CHO cells Ml3nSpVv[3Srb36gZZN{[Xl? M1r0NmlvcGmkaYTpc44hd2ZiaIXtZY4hTVKJIHX4dJJme3OnZDDpckBEUE9iY3XscJMh[nlid3jvcIUh[2WubDDwZZRkcCClbHHtdEB1\WOqbnnxeYUtKEmFNUC9NVAvPDdzMzFOwG0> Mn\pNVg1PDh|NEK=
BESM cells NFT2OpBEgXSxdH;4bYNqfHliYYPzZZk> NWi0bG9uQDhiaB?= MVTDfZRwfG:6aXPpeJkh[WejaX7zeEBDTVOPIHPlcIx{KGGodHXyJFg5KGi{czDifUBJXFNiYYPzZZktKEWFNUC9N|Eh|ryP MUGyNFU1PzhzOR?=

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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
in solvent
Synonyms BM-14190, SKF 105517

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03879629 Not yet recruiting Breast Cancer Mayo Clinic|National Cancer Institute (NCI) May 2019 Phase 2
NCT03879629 Not yet recruiting Breast Cancer Mayo Clinic|National Cancer Institute (NCI) May 2019 Phase 2
NCT03776955 Not yet recruiting Cirrhoses Liver|Oesophageal Varices King''s College Hospital NHS Trust|King''s College London|Guy''s and St Thomas'' NHS Foundation Trust|St George''s University Hospitals NHS Foundation Trust|Cardiff University|Brighton and Sussex University Hospitals NHS Trust April 2019 Phase 4
NCT03538015 Not yet recruiting Hypoglycemia Unawareness Owen Chan PhD|University of Utah April 2019 Phase 2
NCT03538015 Not yet recruiting Hypoglycemia Unawareness Owen Chan PhD|University of Utah April 2019 Phase 2
NCT03775096 Not yet recruiting REM Sleep Behavior Disorder|Pre-motor Parkinson Disease|Symptomatic Parkinson Disease Michele Tagliati MD|Cedars-Sinai Medical Center April 1 2019 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID