(R)-Carvedilol is an optically active and R-enantiomer of Carvedilol, which is a nonselective ß-adrenergic blocker with a1-blocking activity. It treats congestive heart failure by acting as an antihypertensive medication./p>
Physicochemical Properties
| Molecular Formula | C₂₄H₂₆N₂O₄ |
| Molecular Weight | 406.47 |
| Exact Mass | 406.189 |
| CAS # | 95093-99-5 |
| Related CAS # | Carvedilol;72956-09-3; (S)-Carvedilol; 95094-00-1; Carvedilol phosphate hemihydrate; 610309-89-2; (R)-Carvedilol-d4; 2747915-92-8 |
| PubChem CID | 185394 |
| Appearance | White to off-white solid |
| Density | 1.25g/cm3 |
| Boiling Point | 655.2ºC at 760 mmHg |
| Melting Point | 114-115ºC |
| Flash Point | 350.1ºC |
| Index of Refraction | 1.657 |
| LogP | 4.128 |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 5 |
| Rotatable Bond Count | 10 |
| Heavy Atom Count | 30 |
| Complexity | 508 |
| Defined Atom Stereocenter Count | 1 |
| SMILES | O(C1C=CC=C2C=1C1C=CC=CC=1N2)C[C@H](O)CNCCOC1C=CC=CC=1OC |
| InChi Key | OGHNVEJMJSYVRP-QGZVFWFLSA-N |
| 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 |
| Chemical Name | (2R)-1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol |
| Synonyms | (R)-Carvedilol; (R) Carvedilol; (R)-BM 14190 |
| HS Tariff Code | 2934.99.9001 |
| 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) |
Biological Activity
| Targets | β/α-1 adrenergic receptor |
| References |
[1]. 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. |
| Additional Infomation | See also: Carvedilol (annotation moved to). |
Solubility Data
| Solubility (In Vitro) | DMSO: ~220 mg/mL (~541.3 mM) |
| 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. 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. 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 corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
| 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 |