| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
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| ln Vitro |
When compared to (R)-carvedilol, (S)-carvedilol has a beta-blocking action that is about 100 times stronger, and both enantiomers have the same potency as alpha-blockers [1]. By raising the activities of superoxide dismutase and catalase, decreasing the levels of reactive oxygen species and malondialdehyde through PI3K, and enhancing superoxide dismutase and catalase, (S)-Carvedilol dramatically attenuates doxorubicin (DOX)-induced cell death and apoptosis. AKT/eNO synthase pathway modifications, decreased mitochondrial membrane potential, and oxidative stress response in vitro [1]. In HUVEC, treatment with (S)-Carvedilol markedly increased the expression level of p-eNOS [1].
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| ADME/Pharmacokinetics |
Metabolism / Metabolites
(s)-(-)-carvedilol has known human metabolites that include 4'-hydroxy-carvedilol, 8-hydroxy-carvedilol, 5'-hydroxy-carvedilol, and O-Desmethylcarvedilol. |
| 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.
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| Molecular Formula |
C24H26N2O4
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|---|---|
| Molecular Weight |
406.47424
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| Exact Mass |
406.189
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| CAS # |
95094-00-1
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| Related CAS # |
Carvedilol;72956-09-3;(R)-Carvedilol;95093-99-5;Carvedilol phosphate hemihydrate;610309-89-2;(S)-Carvedilol-d4;2747915-23-5
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| PubChem CID |
185395
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| Appearance |
Off-white to gray solid powder
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| Density |
1.25 g/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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| 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
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| SMILES |
O(C1C=CC=C2C=1C1C=CC=CC=1N2)C[C@@H](O)CNCCOC1C=CC=CC=1OC
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| InChi Key |
OGHNVEJMJSYVRP-KRWDZBQOSA-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-/m0/s1
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| Chemical Name |
(2S)-1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol
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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 : ~200 mg/mL (~492.04 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (12.30 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 50.0 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 mg/mL (12.30 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 50.0 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 mg/mL (12.30 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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