| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| Other Sizes |
| Targets |
β/α-1 adrenergic receptor
(R)-Carvedilol targets β-adrenergic receptors as a nonselective blocker and α1-adrenergic receptors as a blocker. By blocking these receptors, it reduces sympathetic nervous system activity, leading to decreased heart rate, cardiac output, and blood pressure. Its α1-blocking activity contributes to vasodilation. |
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| ln Vitro |
In vitro, (R)-Carvedilol is characterized as a nonselective β-adrenergic blocker with α1-blocking activity. It is the optically active R-enantiomer of Carvedilol. Its activity makes it a valuable tool for studying adrenergic receptor function and its role in cardiovascular physiology.
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| ln Vivo |
In vivo, (R)-Carvedilol is an antihypertensive agent used in the treatment of congestive heart failure. As a nonselective β-blocker with α1-blocking activity, it reduces blood pressure and improves cardiac function. Its efficacy has been demonstrated in clinical studies.
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| Enzyme Assay |
In vitro receptor binding assays for (R)-Carvedilol involve measuring its affinity for β1, β2, and α1 adrenergic receptors. Radioligand binding studies using ³H-CGP12177 (for β) or ³H-prazosin (for α1) are performed on membranes from cells expressing the receptors. Ki values are calculated. Functional assays measure its ability to antagonize agonist-induced signaling.
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| Cell Assay |
For in vitro cell-based assays, cells expressing adrenergic receptors are cultured and treated with (R)-Carvedilol at various concentrations. Receptor antagonism is confirmed by its ability to block agonist-induced cAMP accumulation (for β) or calcium signaling (for α1). Cell viability is assessed by standard assays. Its vasodilating properties can be assessed in isolated vascular ring preparations.
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| Animal Protocol |
In vivo animal studies with (R)-Carvedilol are conducted in models of hypertension and heart failure. The compound is administered orally to animals. Blood pressure and heart rate are measured. Cardiac function is assessed by echocardiography. Its effects on vascular resistance and cardiac remodeling are evaluated.
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| ADME/Pharmacokinetics |
(R)-Carvedilol (CAS: 95093-99-5) has a molecular weight of 406.47 g/mol and a molecular formula of C24H26N2O4. Appearance: solid powder. Purity: ≥98%. Synonyms: (+)-Carvedilol. Solubility: DMSO. Storage: powder -20°C 3 years, 4°C 2 years.
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| Toxicity/Toxicokinetics |
(R)-Carvedilol is a research compound and is not approved for human therapeutic use as a single enantiomer. As an adrenergic blocker, it may have effects on cardiovascular function. Standard laboratory safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
See also: Cavidilol (notes moved to).
(R)-Carvedilol is the optically active R-enantiomer of Carvedilol, a nonselective β-adrenergic blocker with α1-blocking activity. It has the CAS number 95093-99-5 and a molecular weight of 406.47 g/mol. It is an antihypertensive agent. It is not FDA-approved as a single enantiomer and is intended for research use only. |
| Molecular Formula |
C₂₄H₂₆N₂O₄
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|---|---|
| Molecular Weight |
406.47
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| Exact Mass |
406.189
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| CAS # |
95093-99-5
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| Related CAS # |
Carvedilol;72956-09-3; (S)-Carvedilol; 95094-00-1; Carvedilol phosphate hemihydrate; 610309-89-2; (R)-Carvedilol-d4; 2747915-92-8
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| PubChem CID |
185394
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| Appearance |
White to off-white solid
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| Density |
1.25g/cm3
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| Boiling Point |
655.2ºC at 760 mmHg
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| Melting Point |
114-115ºC
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| Flash Point |
350.1ºC
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| Index of Refraction |
1.657
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| LogP |
4.128
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
30
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| Complexity |
508
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| Defined Atom Stereocenter Count |
1
|
| SMILES |
O(C1C=CC=C2C=1C1C=CC=CC=1N2)C[C@H](O)CNCCOC1C=CC=CC=1OC
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| InChi Key |
OGHNVEJMJSYVRP-QGZVFWFLSA-N
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| InChi Code |
InChI=1S/C24H26N2O4/c1-28-21-10-4-5-11-22(21)29-14-13-25-15-17(27)16-30-23-12-6-9-20-24(23)18-7-2-3-8-19(18)26-20/h2-12,17,25-27H,13-16H2,1H3/t17-/m1/s1
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| Chemical Name |
(2R)-1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol
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| Synonyms |
(R)-Carvedilol; (R) Carvedilol; (R)-BM 14190
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~220 mg/mL (~541.3 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5.5 mg/mL (13.53 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 55.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 5.5 mg/mL (13.53 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 55.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5.5 mg/mL (13.53 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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