| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
Carvedilol phosphate hemihydrate targets beta-adrenergic receptors (β1, β2) and alpha-1 (α1) adrenergic receptors as a nonselective blocker. It inhibits LDL oxidation with an IC50 of 3.8 μM. The compound inhibits lipid peroxidation with an IC50 of 5 μM. It is an autophagy inducer that inhibits the NLRP3 inflammasome. The compound has cardioprotective effects.
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| ln Vitro |
With an IC50 of 28 μM, carvingilol prevents activated human neutrophils from producing superoxide in vitro. With an IC50 of 25 μM, carvingilol scavenges oxygen free radicals in cell-free systems [2].
In vitro, Carvedilol phosphate hemihydrate inhibits LDL oxidation with an IC50 of 3.8 μM. It inhibits lipid peroxidation with an IC50 of 5 μM. Superoxide generation by activated human neutrophils is inhibited by Carvedilol with an IC50 of 28 μM. The compound scavenges oxygen free radicals in a cell-free system with an IC50 of 25 μM. It is an autophagy inducer that inhibits the NLRP3 inflammasome. |
| ln Vivo |
In vivo, Carvedilol phosphate hemihydrate is used primarily in the treatment of hypertension and heart failure. It has potential use in angina and congestive heart failure. Its inhibitory action at adrenergic receptors slows heart rhythm, decreasing force, pressure, and cardiac workload. The compound is a cardioprotective α1- and β1/2-adrenergic receptor inhibitor.
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| Enzyme Assay |
In vitro receptor binding assays for Carvedilol phosphate hemihydrate involve measuring affinity for beta-1, beta-2, and alpha-1 adrenergic receptors. Radioligand binding displacement studies are performed using membranes from cells expressing these receptors. LDL oxidation inhibition is assessed by measuring oxidized LDL formation. Lipid peroxidation inhibition is measured using standard lipid peroxidation assays. NLRP3 inflammasome inhibition is assessed by measuring IL-1β release. Assays are performed in appropriate buffer systems with positive controls.
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| Cell Assay |
In vitro cell-based assays for Carvedilol phosphate hemihydrate are conducted in various cell lines. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with the compound at varying concentrations. Autophagy induction is assessed by measuring LC3-II conversion and autophagosome formation. NLRP3 inflammasome inhibition is assessed by measuring caspase-1 activity and IL-1β release. Cell viability is assessed by standard assays. Experiments are performed in triplicate with appropriate positive and negative controls.
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| Animal Protocol |
Carvedilol phosphate hemihydrate in vivo studies are conducted in animal models of hypertension and heart failure. Animals are treated with the compound via oral administration. Blood pressure and heart rate are monitored. For heart failure studies, cardiac function is assessed by echocardiography. Autophagy induction and NLRP3 inflammasome inhibition are assessed in cardiac tissues. Dosing regimens are optimized based on pharmacokinetic data. Animals are monitored for clinical signs. Tissues and blood samples are collected for histopathological and biomarker analysis at study endpoints. Studies are conducted in accordance with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
Carvedilol phosphate hemihydrate (MW 513.48 g/mol, C48H60N4O17P2) is a non-selective beta/alpha-1 blocker. It appears as a solid powder with ≥98% purity. The compound should be stored dry, dark, and at -20°C for 1 year. Pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution have been characterized in clinical studies. The compound is used in cardiovascular research.
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| Toxicity/Toxicokinetics |
Carvedilol phosphate hemihydrate is generally well-tolerated at therapeutic doses. The compound is a non-selective beta/alpha-1 blocker with established safety profiles for hypertension and heart failure treatment. No significant adverse effects have been reported in the available literature at research-use concentrations. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation is available from clinical use data.
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| References |
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| Additional Infomation |
Carvedilol phosphate is the phosphate form of carvedilol, a racemic mixture belonging to the adrenergic blocker class. It possesses antihypertensive activity but lacks intrinsic sympathomimetic activity. The S enantiomer of carvedilol nonselectively binds to and blocks β-adrenergic receptors, thereby producing negative inotropic and negative chronotropic effects, leading to decreased cardiac output. Furthermore, both enantiomers of carvedilol bind to and block α1-adrenergic receptors, thereby causing vasodilation and reducing peripheral vascular resistance.
See also: Carvedilol (containing the active ingredient). Carvedilol phosphate hemihydrate is a non-selective beta-adrenergic blocker with alpha-1 blocking activity used in hypertension and heart failure treatment. It inhibits LDL oxidation (IC50 = 3.8 μM) and lipid peroxidation (IC50 = 5 μM). The compound is an autophagy inducer that inhibits the NLRP3 inflammasome. Its molecular formula is C48H60N4O17P2 with a molecular weight of 513.48 g/mol. All applications are limited to non-human research use. |
| Molecular Formula |
2(C24H26N2O4).2(H3PO4).H2
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|---|---|
| Molecular Weight |
1026.97
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| Exact Mass |
1026.342
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| CAS # |
610309-89-2
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| Related CAS # |
Carvedilol;72956-09-3;(S)-Carvedilol;95094-00-1;(R)-Carvedilol;95093-99-5;Carvedilol metabolite 4-Hydroxyphenyl Carvedilol;142227-49-4
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| PubChem CID |
11954344
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| Appearance |
White to off-white solid powder
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| Boiling Point |
655.2ºC at 760 mmHg
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| Flash Point |
350.1ºC
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| LogP |
3.136
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| Hydrogen Bond Donor Count |
13
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| Hydrogen Bond Acceptor Count |
19
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| Rotatable Bond Count |
20
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| Heavy Atom Count |
71
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| Complexity |
557
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=P(OO)=O.OC(CNCCOC1=CC=CC=C1OC)COC2=CC=CC(N3)=C2C4=C3C=CC=C4.[HH].[0.5H2O]
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| InChi Key |
LHNYXTULDSJZRB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/2C24H26N2O4.2H3O4P.H2O/c2*1-28-21-10-4-5-11-22(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;2*1-5(2,3)4;/h2*2-12,17,25-27H,13-16H2,1H3;2*(H3,1,2,3,4);1H2
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| Chemical Name |
1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol;phosphoric acid;hydrate
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9737 mL | 4.8687 mL | 9.7374 mL | |
| 5 mM | 0.1947 mL | 0.9737 mL | 1.9475 mL | |
| 10 mM | 0.0974 mL | 0.4869 mL | 0.9737 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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