Carvedilol (Synonyms: BM 14190)

Name: Carvedilol
Brand: MedChemExpress
SKU: HY-B0006
Rating: 5.0 (6 reviews)

Cat. No.: HY-B0006 Purity: 99.89%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

Carvedilol Chemical Structure

CAS No. : 72956-09-3

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
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5 g		Get quote

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Based on 6 publication(s) in Google Scholar

Other Forms of Carvedilol:

Carvedilol metabolite 4-Hydroxyphenyl Carvedilol Get quote
(S)-Carvedilol Get quote
(R)-Carvedilol Get quote
Carvedilol-d₃ Get quote
Carvedilol-d₄ Get quote
Carvedilol-d₅ Get quote
Carvedilol phosphate hemihydrate Get quote
Carvedilol (Standard) Get quote

6 Publications Citing Use of MCE Carvedilol

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α adrenergic receptor β adrenergic receptor

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	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	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
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.

72956-09-3

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
10 mM	0.2460 mL	1.2301 mL	2.4602 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
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

mg/kg

Animal weight
(per animal)

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: 99.89%

Select Batch:

Data Sheet (276 KB) SDS (398 KB)

COA (251 KB) LCMS (268 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
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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Carvedilol (Synonyms: BM 14190)

Customer Review

Other Forms of Carvedilol:

Carvedilol Related Antibodies

6 Publications Citing Use of MCE Carvedilol

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Adrenergic Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Carvedilol Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Carvedilol Related Classifications

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