(R)-Carvedilol
Based on 1 Customer Validation
(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.
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- Purity: 98.78%
- CAS No.: 95093-99-5
- 화학식: C24H26N2O4
- 분자량:406.47
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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β adrenergic receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.9 μM
Compound: 4
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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
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[PMID: 27546834] |
| CHO | IC50 |
2.3 μM
Compound: 4
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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
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[PMID: 27546834] |
(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 (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.
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Animal Model:RyR2-R4496C heterozygous mutant mice (129/SvImJ background) with catecholaminergic polymorphic ventricular tachycardia (CPVT)[2]
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Dosage:0.4 mg/kg, 0.8 mg/kg, 1.6 mg/kg, 3.2 mg/kg
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Administration:Intraperitoneal injection, 5 days
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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.
Chemical Information
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CAS No. 95093-99-5
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Appearance Solid
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분자량 406.47
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화학식 C24H26N2O4
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Color White to off-white
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SMILES
O[C@H](CNCCOC1=CC=CC=C1OC)COC2=CC=CC(N3)=C2C4=C3C=CC=C4
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Synonyms
(R)-BM 14190
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Wu T, et al. Protective effects of S-carvedilol on doxorubicin-induced damages to human umbilical vein endothelial cells and rats. J Appl Toxicol. 2019 Aug;39(8):1233-1244. [Content Brief]
[2]. Zhang J, et al. Non-β-blocking R-carvedilol enantiomer suppresses Ca2+ waves and stress-induced ventricular tachyarrhythmia without lowering heart rate or blood pressure. Biochem J. 2015 Sep 1;470(2):233-42. [Content Brief]
[3]. Sardar PK, et al. Oral delivery of the non-β-blocking R-carvedilol enantiomer for skin cancer chemoprevention in SKH-1 mice. AAPS Open. 2025;11:1. [Content Brief]
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 |
(R)-Carvedilol Related Classifications
HY-B0006C Related Classifications
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