Carvedilol

Catalog No.S1831 Batch:S183102

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Technical Data

Formula

C24H26N2O4
Molecular Weight 406.47 CAS No. 72956-09-3
Solubility (25°C)* In vitro DMSO 81 mg/mL (199.27 mM)
Ethanol 4 mg/mL (9.84 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 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]

Protocol (from reference)

Selleck's Carvedilol has been cited by 9 publications

Propafenone facilitates mitochondrial-associated ferroptosis and synergizes with immunotherapy in melanoma [ J Immunother Cancer, 2024, 12(11)e009805] PubMed: 39581704
Carvedilol Phenocopies PGC-1α Overexpression to Alleviate Oxidative Stress, Mitochondrial Dysfunction and Prevent Doxorubicin-Induced Toxicity in Human iPSC-Derived Cardiomyocytes [ Antioxidants (Basel), 2023, 12(8)1585] PubMed: 37627583
Carvedilol Phenocopies PGC-1α Overexpression to Alleviate Oxidative Stress, Mitochondrial Dysfunction and Prevent Doxorubicin-Induced Toxicity in Human iPSC-Derived Cardiomyocytes [ Antioxidants (Basel), 2023, 12(8)1585] PubMed: 37627583
The novel anti-colitic effect of β-adrenergic receptors via modulation of PS1/BACE-1/Aβ axis and NOTCH signaling in an ulcerative colitis model [ Front Pharmacol, 2022, 13:1008085] PubMed: 36386153
Screening of GPCR drugs for repurposing in breast cancer [ Front Pharmacol, 2022, 13:1049640] PubMed: 36561339
Identification of amitriptyline HCl, flavin adenine dinucleotide, azacitidine and calcitriol as repurposing drugs for influenza A H5N1 virus-induced lung injury. [ PLoS Pathog, 2020, 16;16(3):e1008341] PubMed: 32176725
Evaluation of cardioprotective effect of aqueous extract of Allium cepa Linn. bulb on isoprenaline-induced myocardial injury in Wistar albino rats [ Res Pharm Sci, 2016, 11(5):419-427] PubMed: 27920825
Evaluation of cardioprotective effect of aqueous extract of Garcinia indica Linn. fruit rinds on isoprenaline-induced myocardial injury in Wistar albino rats [ Res Pharm Sci, 2015, 10(5):388-96] PubMed: 26752987
Evaluation of cardioprotective effect of aqueous extract of Garcinia indica Linn. fruit rinds on isoprenaline-induced myocardial injury in Wistar albino rats [Patel KJ, et al. Res Pharm Sci, 2015, 10(5):388-96] PubMed: 26752987

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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