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100mg |
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250mg |
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500mg |
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1g |
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2g |
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5g |
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10g |
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Purity: ≥98%
Carvedilol (BM-14190, SKF-105517; Coreg; Dilatrend; Carvedilolum; Eucardic; Kredex; Querto; Coropres) is a non-selective beta blocker/alpha-1 blocker with antihypertensive effects. It has been used to treat high blood pressure and congestive heart failure (CHF). Using an IC50 of 8.1 mM, carvingilol rapidly suppresses Fe(++)-initiated lipid peroxidation as measured by thiobarbituric acid reactive substance (TBARS) in rat brain homogenate. With an IC50 of 17.6 mM, carvingilol guards against Fe(++)-induced alpha-tocopherol depletion in rat brain homogenate. With an IC50 of 25 mM, carvingilol dose-dependently reduces the DMPO-OH signal's intensity.
Targets |
lipid peroxidation ( IC50 = 5 μM ); Autophagy; β/α-1 adrenergic receptor
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
In rat brain homogenate, carvedilol significantly reduced Fe2+-induced lipid peroxidation with an IC50 of 8.1 μM. Carvedilol had an IC50 of 17.6 μM and prevented Fe2+-induced α-tocopherol depletion in rat brain homogenate. With an IC50 of 25 μM, carvingilol reduced the DMPO-OH signal's intensity in a dose-dependent manner. Carvedilol inhibited the migration, proliferation, and formation of neointimal tissue in vascular smooth muscle cells after vascular injury. The mitogenesis that was stimulated by platelet-derived growth factor, epidermal growth factor, thrombin, and serum was inhibited in human cultured pulmonary artery vascular smooth muscle cells by carvedilol (0.1–10 μM), with IC50 values ranging from 0.3 to 2.0 μM. Platelet-derived growth factor-induced vascular smooth muscle cell migration was inhibited by carvedilol with an IC50 value of 3 μM, concentration-dependently.
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Animal Protocol |
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References |
Molecular Formula |
C24H26N2O4
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Molecular Weight |
406.47
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Exact Mass |
406.19
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Elemental Analysis |
C, 70.92; H, 6.45; N, 6.89; O, 15.74
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CAS # |
72956-09-3
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Related CAS # |
(S)-Carvedilol; 95094-00-1; (R)-Carvedilol; 95093-99-5; Carvedilol-d4; 1133705-56-2; Carvedilol metabolite 4-Hydroxyphenyl Carvedilol; 142227-49-4; Carvedilol phosphate hemihydrate; 610309-89-2; Carvedilol-d3; 1020719-25-8; Carvedilol-d5; 929106-58-1
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Appearance |
Solid powder
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SMILES |
COC1=CC=CC=C1OCCNCC(COC2=CC=CC3=C2C4=CC=CC=C4N3)O
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InChi Key |
OGHNVEJMJSYVRP-UHFFFAOYSA-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
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Chemical Name |
1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol
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Synonyms |
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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 |
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.15 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 25.0 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: 2.5 mg/mL (6.15 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 25.0 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: ≥ 2.5 mg/mL (6.15 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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT03736265 | Active Recruiting |
Drug: Carvedilol | Cirrhosis, Liver Portal Hypertension |
Beijing Friendship Hospital | October 9, 2017 | Not Applicable |
NCT04023110 | Active Recruiting |
Drug: Carvedilol | Cardiotoxicity Breast Cancer |
Abramson Cancer Center at Penn Medicine |
August 9, 2019 | Phase 1 |
NCT01608893 | Active Recruiting |
Drug: Carvedilol Drug: Metoprolol |
Atrial Fibrillation | University of Calgary | May 2012 | Not Applicable |
NCT02717507 | Active Recruiting |
Other: Pharmacological Study Drug: Carvedilol |
Malignant Solid Neoplasm | Children's Oncology Group | April 4, 2016 | Phase 2 |
NCT02993198 | Active Recruiting |
Drug: Carvedilol | HER2 Positive Breast Cancer Cardiovascular Abnormalities |
Northwestern University | April 2015 | Phase 2 |
β2AR phosphorylation stimulated by carvedilol. Proc Natl Acad Sci U S A . 2007 Oct 16;104(42):16657-62. td> |
β-arrestin2-GFP translocation to the β2AR-V2R and receptor internalization stimulated by carvedilol. HEK-293 cells transiently expressing the β2AR-V2R chimera were stimulated for 2 min with either isoproterenol (Iso), carvedilol (Carv), or propranolol (Prop). Proc Natl Acad Sci U S A . 2007 Oct 16;104(42):16657-62. td> |