Carteolol HCl (Synonyms: NSC 300906, OPC 1085) |
| Catalog No.GC16395 |
Carteolol HCl (clorhidrato de OPC-1085) es un bloqueador beta no selectivo que se usa para tratar el glaucoma.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 51781-21-6
Sample solution is provided at 25 µL, 10mM.
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Beta-adrenergic antagonist are an important class of drugs for the treatment of various heart diseases, such as high blood pressure, insufficiency of blood flow to the heart muscle, irregular heart beat, thickened heart muscle, and decreased ability of the heart to empty or fill normally. β-Blockers can also be used to treat migraine headache and increased eye pressure (glaucoma). Carteolol is a nonselective beta-adrenoceptor antagonist.
In vitro: Previous findings demonstrate that carteolol, unlike xamoterol, is a nonconventional partial agonist, which causes agonistic effects via interaction with the low-affinity propranolol-resistant site of β1-adrenoceptors and antagonistic actions by the high-affinity site of the same receptors [1].
In vivo: Both 8-OH carteolol and carteolol suppressed the water-load induced intraocular pressure (IOP) rise in rabbits. 8-OH carteolol was more effective in suppressing water-load induced IOP rise in rabbits compared with carteolol on equimolar basis. Both 8-OH carteololand carteolol caused a significant decrease in IOP in monkeys. 8-OH carteolol was estimated to be more potent than carteolol in lowering IOP on equimolar basis in monkeys [2].
Clinical trial: The new alginate formulation of long-acting carteolol 1% given once daily is as effective as standard 1% carteolol given twice daily, with no meaningful differences regarding safety. The new alginate formulation of long-acting 1% carteolol given once a day is effective and well tolerated by glaucoma patients requiring chronic treatment [3].
Reference:
[1] Maura Floreani, Guglielmina Froldi, Luigi Quintieri, Katia Varani, Pier Andrea Borea, Maria Teresa Dorigo and Paola Dorigo. In Vitro Evidence That Carteolol Is a Nonconventional Partial Agonist of Guinea Pig Cardiac β1-Adrenoceptors: A Comparison with Xamoterol. JPET 315:1386–1395, 2005
[2] Sugiyama K, Enya T, Kitazawa Y. Ocular hypotensive effect of 8-hydroxycarteolol, a metabolite of carteolol. Int Ophthalmol. 1989 Jan;13(1-2):85-9.
[3] Trinquand C, Romanet JP, Nordmann JP, Allaire C; Groupe d'étude. Efficacy and safety of long-acting carteolol 1% once daily. A double-masked, randomized study. J Fr Ophtalmol. 2003 Feb;26(2):131-6.
| Cas No. | 51781-21-6 | SDF | |
| Sinónimos | NSC 300906, OPC 1085 | ||
| Chemical Name | 5-(3-(tert-butylamino)-2-hydroxypropoxy)-3,4-dihydroquinolin-2-ol hydrochloride | ||
| Canonical SMILES | CC(C)(NCC(O)COC1=CC=CC2=C1CCC(O)=N2)C.Cl | ||
| Formula | C16H25ClN2O3 | M.Wt | 328.83 |
| Solubility | ≥ 16.4mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.0411 mL | 15.2054 mL | 30.4109 mL |
| 5 mM | 0.6082 mL | 3.0411 mL | 6.0822 mL |
| 10 mM | 0.3041 mL | 1.5205 mL | 3.0411 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 11 reference(s) in Google Scholar.)
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