Cat. No.: HY-B0006

Carvedilol

(Synonyms: BM 14190)

14 Cited Publications

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Based on 14 publication(s) in Google Scholar

Carvedilol (BM 14190) is a non-selective β/α-1 blocker. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC₅₀ of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome.

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Pureté: 99.98%
CAS No.: 72956-09-3
Formule: C₂₄H₂₆N₂O₄
Masse moléculaire:406.47

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Carvedilol Chemical Structure

CAS No.: 72956-09-3

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Essai clinique
Chemical Information
Publications (14)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Carvedilol (BM 14190) is a non-selective β/α-1 blocker^[1]. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC₅₀ of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure^[2]. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome^[3].

IC₅₀ & Target

β/α-1 adrenergic receptor^[1]
IC50: 5 μM (lipid peroxidation)^[2]
Autophagy^[3]

Voir tous les produits spécifiques à Isoform Adrenergic Receptor :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	13.01 μM Compound: Carvedilol	Antiproliferative activity against human A375 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human A375 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 32216987]
HEK293	IC₅₀	1.6 μM Compound: 38	Inhibition of of human TREK1 expressed in HEK293 cells assessed as reduction in channel currents Inhibition of of human TREK1 expressed in HEK293 cells assessed as reduction in channel currents	[PMID: 26588045]
HEK293	IC₅₀	12 μM Compound: Carvedilol	Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method	[PMID: 21030469]
HEK293	IC₅₀	15.9 μM Compound: 1	Inhibition of RyR2 R4496C mutant (unknown origin)-mediated store-overload induced calcium release expressed in HEK293 cells after 8 to 10 mins by fura-2/AM dye-based fluorescence assay Inhibition of RyR2 R4496C mutant (unknown origin)-mediated store-overload induced calcium release expressed in HEK293 cells after 8 to 10 mins by fura-2/AM dye-based fluorescence assay	[PMID: 24124794]
HEK293	IC₅₀	27 μM Compound: Carvedilol	Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method	[PMID: 21030469]
HEK293	IC₅₀	3.4 μM Compound: Carvedilol	Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay	[PMID: 28230985]
HEK293	IC₅₀	7.5 μM Compound: carvedilol	Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	7.6 μM Compound: 38	Inhibition of of TREK2 (unknown origin) expressed in HEK293 cells assessed as reduction in channel currents Inhibition of of TREK2 (unknown origin) expressed in HEK293 cells assessed as reduction in channel currents	[PMID: 26588045]
HEK293	IC₅₀	92.4 μM Compound: carvedilol	Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
L02	IC₅₀	85 μM Compound: SYSU-20532S	Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay	10.1039/C3MD00397C
NIH-3T3-G185	IC₅₀	4.6 μM Compound: Carvedilol	TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	6 μM Compound: Carvedilol	TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	6.6 μM Compound: Carvedilol	TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells	[PMID: 11716514]
SK-MEL-28	IC₅₀	15.55 μM Compound: Carvedilol	Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 32216987]
SK-MEL-5	IC₅₀	13.73 μM Compound: Carvedilol	Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 32216987]

In Vitro

Superoxide generation by activated human neutrophils in vitro is inhibited by Carvedilol with an IC₅₀ of 28 μM. Carvedilol is shown to scavenge oxygen free radicals in a cell-free system with an IC₅₀ of 25 μM^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 72956-09-3
Appearance Solid
Masse moléculaire 406.47
Formule C₂₄H₂₆N₂O₄
Color White to off-white
SMILES

OC(CNCCOC1=CC=CC=C1OC)COC2=CC=CC(N3)=C2C4=C3C=CC=C4
Synonyms

BM 14190
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (14)

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Redox Biol

Oxidative stress promotes lipid-laden macrophage formation via CYP1B1. [Abstract]

2024 Dec 21:79:103481. PMID: 39721495

Carvedilol purchased from MedChemExpress. Usage Cited in: Redox Biol. 2024 Dec 21:79:103481. [Abstract]

U937 macrophages cultured with or without 5 % CSE were treated with 5 μM, 10 μM, or 20 μM Carvedilol (Carv) for 3 days. LLM formation was determined using ORO staining.
Free Radic Biol Med

IL-6/gp130/STAT3 signaling contributed to the activation of the PERK arm of the unfolded protein response in response to chronic β-adrenergic stimulation. [Abstract]

2023 Aug 20:205:163-174. PMID: 37307935
Cell Rep

A central amygdala-locus coeruleus pathway mediating pain under chronic stress. [Abstract]

2026 Jun 18;45(7):117570. PMID: 42313564
Cell Rep

Carvedilol sensitizes chemotherapy by targeting STING to boost anti-tumor immunity. [Abstract]

2025 Apr 16;44(5):115572. PMID: 40249703

Carvedilol purchased from MedChemExpress. Usage Cited in: Cell Rep. 2025 Apr 16;44(5):115572. [Abstract]

Real-time qPCR measurement of Ifnb1 and Cxcl10 transcripts in mouse peritoneal macrophages treated with cGAMP (1 μg/mL) and Digitonin (10 μg/mL) for indicated times in the presence of DMSO or Carvedilol (10 μM).

Carvedilol purchased from MedChemExpress. Usage Cited in: Cell Rep. 2025 Apr 16;44(5):115572. [Abstract]

ELISA of IFN-β and CXCL10 production in mouse peritoneal macrophages treated with cGAMP or ISD for 12 h in the presence of DMSO or Carvedilol (10 μM).

Carvedilol purchased from MedChemExpress. Usage Cited in: Cell Rep. 2025 Apr 16;44(5):115572. [Abstract]

Immunoblotting of the indicated signaling molecules in mouse peritoneal macrophages treated with cGAMP or ISD in the presence of DMSO or Carvedilol (10 μM) for indicated times.

Carvedilol purchased from MedChemExpress. Usage Cited in: Cell Rep. 2025 Apr 16;44(5):115572. [Abstract]

Carvedilol (10 μM) enhanced HA-STING but not HA-STING^T263A localizing to ERGIC by Immunofluorescence assay.
Cell Rep

Pharmacological boosting of cGAS activation sensitizes chemotherapy by enhancing antitumor immunity. [Abstract]

2023 Mar 20;42(3):112275. PMID: 36943864
Cells

Redistribution of the SWI/SNF Complex Dictates Coordinated Transcriptional Control over Epithelial-Mesenchymal Transition of Normal Breast Cells through TGF-β Signaling. [Abstract]

2022 Aug 24;11(17):2633. PMID: 36078038
J Pathol

Novel prognostication biomarker adipophilin reveals a metabolic shift in uveal melanoma and new therapeutic opportunities. [Abstract]

2023 Jun;260(2):203-221. PMID: 36825655
ACS Omega

Computational and Experimental Approaches Identify Beta-Blockers as Potential SARS-CoV-2 Spike Inhibitors. [Abstract]

2022 Aug 8;7(32):27950-27958. PMID: 35983371
Biochim Biophys Acta Mol Basis Dis

Both carvedilol and cimetidine alleviate cisplatin-induced nephrotoxicity via downregulating OCT2. [Abstract]

2025 Jun;1871(5):167754. PMID: 40044066
J Nat Prod

Spirocyclic Adduct Formation of Tryptanthrin with Indole Monoamines under Biomimetic Acidic Conditions. [Abstract]

2026 Feb 27;89(2):645-655. PMID: 41680098
J Diabetes Res

Diabetic Cardiomyopathy Uncovered: Transcriptomics, NLRP3, and Carvedilol Mechanisms. [Abstract]

2024 Nov 23:2024:9378405. PMID: 39619569
Cardiooncology

Breast cancer progression in the presence of treated and untreated left ventricular dysfunction. [Abstract]

2025 Nov 13;11(1):106. PMID: 41233850
Comput Biol Chem

Targeting quorum sensing in Pseudomonas aeruginosa with high-affinity inhibitors: A high-throughput screening and in-silico analysis. [Abstract]

2025 Aug:117:108419. PMID: 40088808
J Pharm Biomed Anal

Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]

2021 Feb 20:195:113870. PMID: 33453569

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (246.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4602 mL

12.3010 mL

24.6021 mL

5 mM

0.4920 mL

2.4602 mL

4.9204 mL

10 mM

0.2460 mL

1.2301 mL

2.4602 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (6.15 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Eggertsen R, et al. Acute haemodynamic effects of carvedilol (BM 14190), a new combined beta-adrenoceptor blocker and precapillary vasodilating agent, in hypertensive patients. Eur J Clin Pharmacol. 1984;27(1):19-22. [Content Brief]

[2]. Feuerstein GZ, et al. Myocardial protection by the novel vasodilating beta-blocker, carvedilol: potential relevance of anti-oxidant activity. J Hypertens Suppl. 1993 Jun;11(4):S41-8. [Content Brief]

[3]. Wong WT, et al. Repositioning of the β-Blocker Carvedilol as a Novel Autophagy Inducer That Inhibits the NLRP3 Inflammasome. Front Immunol. 2018 Aug 22;9:1920. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4602 mL	12.3010 mL	24.6021 mL	61.5052 mL
	5 mM	0.4920 mL	2.4602 mL	4.9204 mL	12.3010 mL
	10 mM	0.2460 mL	1.2301 mL	2.4602 mL	6.1505 mL
	15 mM	0.1640 mL	0.8201 mL	1.6401 mL	4.1003 mL
	20 mM	0.1230 mL	0.6151 mL	1.2301 mL	3.0753 mL
	25 mM	0.0984 mL	0.4920 mL	0.9841 mL	2.4602 mL
	30 mM	0.0820 mL	0.4100 mL	0.8201 mL	2.0502 mL
	40 mM	0.0615 mL	0.3075 mL	0.6151 mL	1.5376 mL
	50 mM	0.0492 mL	0.2460 mL	0.4920 mL	1.2301 mL
	60 mM	0.0410 mL	0.2050 mL	0.4100 mL	1.0251 mL
	80 mM	0.0308 mL	0.1538 mL	0.3075 mL	0.7688 mL
	100 mM	0.0246 mL	0.1230 mL	0.2460 mL	0.6151 mL

Carvedilol

14 Cited Publications

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Carvedilol

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Publications Citing Use of MedChemExpress (MCE) Carvedilol

Voir tous les produits spécifiques à Isoform Adrenergic Receptor

Activité biologique

Chemical Information

Publications (14)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Carvedilol Related Classifications

HY-B0006 Related Classifications