(R)-Carvedilol是Carvedilol的R-对映体，是一种非选择性α受体阻滞剂，IC50值为89.20μM。
Cas No.:95093-99-5
Sample solution is provided at 25 µL, 10mM.
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(R)-Carvedilol, the R-enantiomer of Carvedilol, is a non-selective α receptor blocker with an IC50 value of 89.20μM [1]. (R)-Carvedilol suppresses Ca2+ waves and stress-induced ventricular tachyarrhythmia without lowering heart rate or blood pressure [2]. (R)-Carvedilol has been widely used to improve the neural damage in mouse models of Alzheimer's disease (AD)[3].
In vitro, (R)-Carvedilol (5μM) treatment for 6 hours significantly inhibited doxorubicin (DOX)-induced cell death in human umbilical vein endothelial cells (HUVECs)[4].
In vivo, (R)-Carvedilol treatment via oral administration at a dose of 20mg/kg/day for 2 weeks significantly inhibited UV-induced skin carcinogenesis in SKH-1 mice, without affecting blood pressure[5]. Oral administration of (R)-Carvedilol at a dose of 3.2mg/kg/day for one month can rescue the excessive neuronal hyperactivity and memory loss in 5×FAD mice[6]. Administering 3.2mg/kg/day of (R)-Carvedilol orally for one month can rescue the memory impairment and neuronal loss in 3×TG-AD mice[7].
References:
[1] Bartsch W, Sponer G, Strein K, et al. Pharmacological characteristics of the stereoisomers of carvedilol[J]. European journal of clinical pharmacology, 1990, 38(Suppl 2): S104-S107.
[2] Zhang J, Zhou Q, Smith C D, et al. Non-β-blocking R-carvedilol enantiomer suppresses Ca2+ waves and stress-induced ventricular tachyarrhythmia without lowering heart rate or blood pressure[J]. Biochemical Journal, 2015, 470(2): 233-242.
[3] Yao J, Chen S R W. R-carvedilol, a potential new therapy for Alzheimer’s disease[J]. Frontiers in Pharmacology, 2022, 13: 1062495.
[4] Wu T, Li H, Lan Q, et al. Protective effects of S‐carvedilol on doxorubicin‐induced damages to human umbilical vein endothelial cells and rats[J]. Journal of Applied Toxicology, 2019, 39(8): 1233-1244.
[5] Sardar P K, Yeung S, Tow R, et al. Oral delivery of the non-β-blocking R-carvedilol enantiomer for skin cancer chemoprevention in SKH-1 mice[J]. AAPS open, 2025, 11(1): 1.
[6] Yao J, Sun B, Institoris A, et al. Limiting RyR2 open time prevents Alzheimer’s disease-related neuronal hyperactivity and memory loss but not β-amyloid accumulation[J]. Cell reports, 2020, 32(12).
[7] Liu Y, Yao J, Song Z, et al. Limiting RyR2 open time prevents Alzheimer's disease‐related deficits in the 3xTG‐AD mouse model[J]. Journal of Neuroscience Research, 2021, 99(11): 2906-2921.
(R)-Carvedilol是Carvedilol的R-对映体，是一种非选择性α受体阻滞剂，IC50值为89.20μM[1]。(R)-Carvedilol能够抑制钙波和应激诱导的室性快速性心律失常，且不降低心率或血压[2]。(R)-Carvedilol已被广泛用于改善阿尔茨海默病（AD）小鼠模型中的神经损伤[3]。
在体外，使用5μM的(R)-Carvedilol处理人脐静脉内皮细胞（HUVECs）6小时，显著抑制了阿霉素（DOX）诱导的细胞死亡[4]。
在体内，每日口服20mg/kg剂量的(R)-Carvedilol，连续2周，显著抑制了SKH-1小鼠中紫外线诱导的皮肤癌发生，且不影响血压[5]。每日口服3.2mg/kg剂量的(R)-Carvedilol，持续一个月，可以挽救5×FAD小鼠中过度的神经元过度活跃和记忆丧失[6]。每日口服3.2mg/kg剂量的(R)-Carvedilol一个月，可以挽救3×TG-AD小鼠的记忆障碍和神经元损失[7]。
| Cell experiment [1]: | |
Cell lines | HUVECs |
Preparation Method | HUVECs were cultured in Dulbecco's minimal Eagle's medium (DMEM) supplemented with 10% fetal bovine serum at 37°C in a 5% CO2 incubator. HUVECs were treated with different concentrations of DOX for 24 hours to induce the cell oxidative injury. The cells were divided as follows: (1) control group: cells incubated with DMEM for 24 hours; (2) DOX group: cells incubated with 2μM DOX for 24 hours; (3) (R)-Carvedilol group (5μM): cells pretreated with 5μM (R)-Carvedilol for 6 hours and then exposed to a final concentration of 2μM DOX for 24 hours. Then, the cell viability was analyzed. |
Reaction Conditions | 5μM; 6h |
Applications | (R)-Carvedilol treatment significantly reduced the cell death of HUVECs induced by DOX. |
| Animal experiment [2]: | |
Animal models | 5×FAD mice |
Preparation Method | 5×FAD mice were housed on a 12hr light/dark cycle with ad libitum access to food and water. (R)-Carvedilol (3.2mg/kg/day), carvedilol (racemic mixture) (3.2mg/kg/day), and vehicle control (DMSO) were delivered to 5×FAD mice in drinking water for one month, starting at different ages before (2 months old) or after (4 months old) the occurrence of AD pathologies. The brain tissues of the mice were collected for analysis. |
Dosage form | 3.2mg/kg/day for 1 month; p.o. |
Applications | (R)-Carvedilol treatment reduced neuronal cell death and dendritic spine loss in 5×FAD mice. |
References: | |
| Cas No. | 95093-99-5 | SDF | |
| 别名 | (R)-卡维地洛; (R)-BM 14190 | ||
| Canonical SMILES | O[C@H](CNCCOC1=CC=CC=C1OC)COC2=CC=CC(N3)=C2C4=C3C=CC=C4 | ||
| 分子式 | C24H26N2O4 | 分子量 | 406.47 |
| 溶解度 | 储存条件 | ||
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4602 mL | 12.301 mL | 24.6021 mL |
| 5 mM | 492 μL | 2.4602 mL | 4.9204 mL |
| 10 mM | 246 μL | 1.2301 mL | 2.4602 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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- Purity: >99.00% Appearance: A solid
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