| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Carteolol is cytotoxic and decreases cell viability in a dose- and time-dependent manner (0–2%; 0-28 hours; HCEC) [1]. In HCEC cells, carteolol (0.25%; 4–12 hours) causes necrotic protein expression and apoptosis [1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: HCEC Tested Concentrations: 0.00390625-2% Incubation Duration: 0, 2, 4, 8, 16, 20, 24 and 28 hrs (hours) Experimental Results: Decrease in cell viability and time at doses above 0.0015625% related way. Western Blot Analysis [1] Cell Types: HCEC Tested Concentrations: 0.25% Incubation Duration: 4, 8 and 12 hrs (hours) Experimental Results: The expression of anti-apoptotic proteins Bcl-2 and Bcl-xL was weakened, and the expression of pro-apoptotic protein Bax was enhanced Bad and Proapoptotic proteins Cyt.c and AIF released from mitochondria. Cell cycle analysis [1] Cell Types: HCEC Tested Concentrations: 0.25% Incubation Duration: 4, 8, 12 hrs (hours) Experimental Results: The number of G1 phase of the cell cycle increased, and the number of S phase diminished. |
| ADME/Pharmacokinetics |
Metabolism/Metabolites
Liver. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Lactation Use Currently, there are no data on the use of carteolol during lactation. Because carteolol can be excreted in breast milk in large quantities, it is recommended to prioritize other beta-adrenergic blockers over oral carteolol during the neonatal period. Infants older than 2 months have more mature renal function and are less likely to be affected. The risk to breastfed infants is low when mothers use carteolol eye drops, but some guidelines indicate that gel formulations are superior to solution formulations. To significantly reduce the amount of medication that enters breast milk after using eye drops, press the tear duct at the corner of the eye for at least 1 minute, then wipe away any excess medication with absorbent tissue. ◉ Impact on Breastfed Infants A study of mothers taking beta-blockers while breastfeeding found a numerically increased number of adverse reactions in mothers taking any beta-blocker, but this was not statistically significant. Although the infants were age-matched to the control group, the age of the affected infants was not specified. None of the mothers took carteolol. Beta-adrenergic blockers, which have similar excretory properties to breast milk, have had adverse effects on breastfed newborns. ◉ Effects on lactation and breast milk A study of six patients with hyperprolactinemia and galactorrhea found no change in serum prolactin levels after beta-adrenergic blockade with propranolol. There are currently no reports on the effects of beta-blockers or carteolol during normal lactation. |
| References |
[1]. Su W, et, al. Dose- and Time-Dependent Cytotoxicity of Carteolol in Corneal Endothelial Cells and the Underlying Mechanisms. Front Pharmacol. 2020 Mar 6;11:202.
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| Additional Infomation |
Carteolol is a quinolone secondary alcohol. It has pharmacological effects as a β-adrenergic antagonist, antihypertensive, antiglaucoma agent, antiarrhythmic, and sympathetic blocker. It is the conjugate base of carteolol (1+). Carteolol is a β-adrenergic antagonist and can be used as an antiarrhythmic, antianginal, antihypertensive, and antiglaucoma agent. Carteolol is a β-adrenergic blocker. The mechanism of action of carteolol is as a β-adrenergic antagonist. Carteolol is a synthetic quinolone derivative, a non-selective β-adrenergic receptor blocker with antiglaucoma activity. After topical instillation, carteolol reduces aqueous humor production, thereby lowering intraocular pressure (IOP). Carteolol is a β-adrenergic antagonist used as an antiarrhythmic, antianginal, antihypertensive, and antiglaucoma agent. See also: Carteolol hydrochloride (salt form). Indications: For the treatment of intraocular hypertension and chronic open-angle glaucoma. Mechanism of Action: The primary mechanism by which carteolol lowers intraocular pressure is likely through reduced aqueous humor production. This process is initiated by non-selective β1 and β2 adrenergic receptor blockade. Pharmacodynamics: Carteolol is a β1 and β2 (non-selective) adrenergic receptor blocker and does not possess significant intrinsic sympathomimetic effects, direct myocardial depressant effects, or local anesthetic (membrane stabilizing) effects. When applied topically to the eye, carteolol lowers elevated intraocular pressure as well as normal intraocular pressure, regardless of whether glaucoma is present. Elevated intraocular pressure is a major risk factor in the pathogenesis of glaucomatous visual field defects and optic nerve damage. Unlike cholinergic drugs known to cause pupillary constriction, carteolol has almost no effect on pupil size or accommodation when lowering intraocular pressure.
|
| Molecular Formula |
C16H24N2O3
|
|---|---|
| Molecular Weight |
292.37336
|
| Exact Mass |
292.179
|
| CAS # |
51781-06-7
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| Related CAS # |
Carteolol hydrochloride;51781-21-6
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| PubChem CID |
2583
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| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.13 g/cm3
|
| Boiling Point |
518.6ºC at 760 mmHg
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| Flash Point |
267.4ºC
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| Index of Refraction |
1.5800 (estimate)
|
| LogP |
2.228
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
21
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| Complexity |
354
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC(C)(NCC(O)COC1=CC=CC2=C1CCC(N2)=O)C
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| InChi Key |
LWAFSWPYPHEXKX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H24N2O3/c1-16(2,3)17-9-11(19)10-21-14-6-4-5-13-12(14)7-8-15(20)18-13/h4-6,11,17,19H,7-10H2,1-3H3,(H,18,20)
|
| Chemical Name |
5-[3-(tert-butylamino)-2-hydroxypropoxy]-3,4-dihydro-1H-quinolin-2-one
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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 | 3.4203 mL | 17.1016 mL | 34.2032 mL | |
| 5 mM | 0.6841 mL | 3.4203 mL | 6.8406 mL | |
| 10 mM | 0.3420 mL | 1.7102 mL | 3.4203 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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