1. GPCR/G Protein Neuronal Signaling Autophagy Anti-infection
  2. Adrenergic Receptor Autophagy Bacterial
  3. Carvedilol

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.

For research use only. We do not sell to patients.

CAS No. : 72956-09-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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500 mg In-stock
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Customer Review

Based on 13 publication(s) in Google Scholar

Top Publications Citing Use of Products

    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.

    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-STINGT263A localizing to ERGIC by Immunofluorescence assay.

    View All Adrenergic Receptor Isoform Specific Products:

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    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]

    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.

    Clinical Trial
    Molecular Weight

    406.47

    Formula

    C24H26N2O4

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4602 mL 12.3010 mL 24.6021 mL
    5 mM 0.4920 mL 2.4602 mL 4.9204 mL
    View the Complete Stock Solution Preparation Table

    * 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    V2

    In Vivo:

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

    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.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • 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.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.98%

    References

    Complete Stock Solution Preparation Table

    * 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.

    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
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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    Carvedilol
    Cat. No.:
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