Carvedilol (Synonyms: BM 14190) |
| カタログ番号GC14769 |
カルベジロール (BM 14190) は、非選択的な β/α-1 ブロッカーです 。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 72956-09-3
Sample solution is provided at 25 µL, 10mM.
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Carvedilol is a non-selective antagonist of α1 and β-adrenergic receptors (ARs) [1]. Adrenergic receptors are a type of G protein-coupled receptors and are the targets for adrenaline and noradrenaline in the sympathetic nervous system [2]. Carvedilol is a multi-purpose antihypertensive agent that can be used to treat congestive heart failure (CHF) and hypertension [3]. Carvedilol is also an autophagy inducer that can inhibit the NLRP3 inflammatory body [4].
In vitro, pre-treatment with Carvedilol (5μM; 18h) can inhibit the quantity and activity of MMP-2 and 9 in human aortic smooth muscle cells (HASMCs) stimulated by TNF-α [5]. Pre-treatment with Carvedilol (1-100μM; 48h) 30 minutes before lipopolysaccharide (LPS) stimulation can inhibit lipid peroxidation and IL-1β production in U937 cells in a dose-dependent manner [6].
In vivo, oral administration of Carvedilol (20mg/kg/day for 3 weeks) significantly reduced the severity of experimental autoimmune myocarditis (EAM) in rats with myocarditis and inhibited the thickening of the left ventricular posterior wall and the mRNA expression of inflammatory cytokines and IL-1β protein in myocarditis, as well as the content of myocardial protein carbonylation and peroxide acidic reaction products [6]. Carvedilol (5, 10mg/kg/day for 6 weeks; gavage) treatment significantly reduced the expression of α-SMA, CD31, CD34 and VWF in carbon tetrachloride-induced fibrotic mice, while also reducing serum levels of MMP-8, VEGF and angiopoietin-2 [7].
References:
[1] Yue T L, Cheng H Y, Lysko P G, et al. Carvedilol, a new vasodilator and beta adrenoceptor antagonist, is an antioxidant and free radical scavenger[J]. Journal of Pharmacology and Experimental Therapeutics, 1992, 263(1): 92-98.
[2] Furchgott R F. The receptors for epinephrine and norepinephrine (adrenergic receptors)[J]. Pharmacological reviews, 1959, 11(2): 429-441.
[3] 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.
[4] 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.
[5] Wu TC, Chen YH, Leu HB, et al. Carvedilol, a pharmacological antioxidant, inhibits neointimal matrix metalloproteinase-2 and -9 in experimental atherosclerosis. Free Radic Biol Med. 2007;43(11):1508-1522.
[6] Yuan Z, Shioji K, Kihara Y, et al. Cardioprotective effects of carvedilol on acute autoimmune myocarditis: anti-inflammatory effects associated with antioxidant property[J]. American Journal of Physiology-Heart and Circulatory Physiology, 2004, 286(1): H83-H90.
[7] Wu Y, Li Z, Xiu A Y, et al. Carvedilol attenuates carbon tetrachloride-induced liver fibrosis and hepatic sinusoidal capillarization in mice[J]. Drug design, development and therapy, 2019: 2667-2676.
| Cell experiment [1]: | |
Cell lines | U937 cells |
Preparation Method | U937 cells, human monoblast cells, were stimulated with 10μg/ml lipopolysaccharide (LPS). Carvedilol was added to the medium 30min before LPS stimulation. After 48h, IL-1β in the medium were assayed using commercially available kits. |
Reaction Conditions | 1-100μM; 48h |
Applications | Pre-treatment with Carvedilol dose-dependently inhibited IL-1β production in U937 cells. |
| Animal experiment [2]: | |
Animal models | Lewis rats induced with acute experimental autoimmune myocarditis |
Preparation Method | The experiment was conducted to analyze the effects of three types of beta-blockers on the cardiac function of rats with acute myocardial infarction (EAM), where both heart rate and blood pressure were affected. Rats with EAM were divided into nine groups for the oral administration of 1) Carvedilol at 10mg·kg–1·day–1 (Car-10, n = 6) Carvedilol at 20mg·kg–1·day–1 (Car-20, n = 7) for 3wk. Normal rats treated with the drugs and vehicle were also prepared. Transthoracic echocardiography was performed on the day before the rats were killed on day 21. At death, macroscopic findings and pericardial effusion were graded. |
Dosage form | 10, 20mg/kg/day for 3 weeks; oral |
Applications | Carvedilol can inhibit the shortening of left ventricular fraction in EAM rats, reduce heart rate, and significantly alleviate the severity of myocarditis. |
References: | |
| Cas No. | 72956-09-3 | SDF | |
| 同義語 | BM 14190 | ||
| Chemical Name | 1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol | ||
| Canonical SMILES | COC1=CC=CC=C1OCCNCC(COC2=CC=CC3=C2C4=CC=CC=C4N3)O | ||
| Formula | C24H26N2O4 | M.Wt | 406.47 |
| 溶解度 | ≥ 40.6mg/mL in DMSO | Storage | Store at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
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Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)
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