2. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel
  3. Adrenergic Receptor Calcium Channel
  4. (R)-Carvedilol

(R)-Carvedilol  (Synonyms: (R)-BM 14190)

Cat. No.: HY-B0006C Purity: 98.78% ee.: 98.97%
COA
SDS
Handling Instructions Technical Support

(R)-Carvedilol ((R)-BM 14190) is the orally active R-isomer of Carvedilol (HY-B0006). (R)-Carvedilol has α-receptor blocking activity but no β-receptor blocking activity. (R)-Carvedilol inhibits spontaneous Ca2+ waves. (R)-Carvedilol inhibits stress-induced ventricular tachycardia and delays the development of UV-induced skin tumors and reduces their malignancy.

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

(R)-Carvedilol

(R)-Carvedilol Chemical Structure

CAS No. : 95093-99-5

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10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of (R)-Carvedilol:

(R)-Carvedilol Related Antibodies

Top Publications Citing Use of Products

View All Adrenergic Receptor Isoform Specific Products:

View All Isoforms
α adrenergic receptor β adrenergic receptor

View All Calcium Channel Isoform Specific Products:

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

(R)-Carvedilol ((R)-BM 14190) is the orally active R-isomer of Carvedilol (HY-B0006). (R)-Carvedilol has α-receptor blocking activity but no β-receptor blocking activity. (R)-Carvedilol inhibits spontaneous Ca2+ waves. (R)-Carvedilol inhibits stress-induced ventricular tachycardia and delays the development of UV-induced skin tumors and reduces their malignancy[1][2][3].

IC50 & Target

β adrenergic receptor

 

Cellular Effect
Cell Line Type Value Description References
CHO IC50
0.9 μM
Compound: 4
Displacement of [125I]-orexin A from human OX2 receptor expressed in CHO cell membranes after 90 mins by scintillation counting
Displacement of [125I]-orexin A from human OX2 receptor expressed in CHO cell membranes after 90 mins by scintillation counting
[PMID: 27546834]
CHO IC50
2.3 μM
Compound: 4
Displacement of [125I]-orexin A from human OX1 receptor expressed in CHO cell membranes after 90 mins by scintillation counting
Displacement of [125I]-orexin A from human OX1 receptor expressed in CHO cell membranes after 90 mins by scintillation counting
[PMID: 27546834]
In Vitro

(R)-Carvedilol (5 μM; 6 h) fails to significantly attenuate Doxorubicin (HY-15142A)-induced death of HUVECs[1].
(R)-Carvedilol (0-30 μM) suppresses spontaneous Ca2+ oscillations in HEK293 cells expressing the catecholaminergic polymorphic ventricular tachycardia (CPVT)-causing RyR2-R4496C mutation[2].
R-carvedilol (1 μM) suppresses spontaneous Ca2+ waves in intact hearts isolated from RyR2-R4496C+/− mice[2].

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

(R)-Carvedilol Related Antibodies
In Vivo

(R)-Carvedilol (6 mg/kg; p.o.; 36 days) fails to improve Doxorubicin-induced myocardial damage, hemodynamic abnormalities (e.g., decreased mean arterial pressure and left ventricular systolic pressure), and oxidative stress (decreased superoxide dismutase and catalase activities, increased reactive oxygen species levels) in rats[1].
(R)-Carvedilol (0.4-3.2 mg/kg/day; i.p.; 5 days) suppresses stress-induced ventricular tachyarrhythmia (VT) in RyR2-R4496C knock-in mice in a dose-dependent manner[2].
(R)-Carvedilol (20 mg/kg; p.o. via drinking water) delays UV-induced skin tumor onset in female SKH-1 mice[3].

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

Animal Model: RyR2-R4496C heterozygous mutant mice (129/SvImJ background) with catecholaminergic polymorphic ventricular tachycardia (CPVT)[2]
Dosage: 0.4 mg/kg, 0.8 mg/kg, 1.6 mg/kg, 3.2 mg/kg
Administration: Intraperitoneal injection, 5 days
Result: Had no significant effect on VT duration induced by Epinephrine (HY-B0447) and Caffeine at 0.4 mg/kg and 0.8 mg/kg.
Reduced the VT duration from 66.4% to 20.8% at 1.6 mg/kg.
Demonstrated a slightly stronger inhibitory effect on VT at a dose of 3.2 mg/kg compared to the 1.6 mg/kg dose.
Did not reduce the heart rate or mean blood pressure compared with the control group.
Molecular Weight

406.47

Formula

C24H26N2O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@H](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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 220 mg/mL (541.25 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
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

×
Volume (final)

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: ≥ 5.5 mg/mL (13.53 mM); Clear solution

    This protocol yields a clear solution of ≥ 5.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (55.0 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: 5.5 mg/mL (13.53 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 5.5 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 (55.0 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: 98.78% ee.: 98.97%

SDS (393 KB)

COA (250 KB) HNMR (215 KB) NP-HPLC (415 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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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(R)-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.

Keywords:

(R)-Carvedilol95093-99-5(R)-BM 14190Adrenergic ReceptorCalcium ChannelBeta ReceptorCa2+ channelsCa channelsβ/α-1vascularcardiactoxicityDoxorubicinDOXInhibitorinhibitorinhibit

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