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| 25mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
Levobetaxolol HCl ((S)-Betaxolol; AL 1577A; Betaxon; AL-1577A) is the hydrochloride salt of Levobetaxolol which is a potent beta-adrenergic receptor inhibitor/beta blocker with antihypertensive effects. Levobetaxolol, the S-isomer of betaxolol, shows a higher affinity at cloned human β1 and β2 receptors with Ki value of 0.76 nM and 32.6 nM, respectively. It is used to treat conditions like glaucoma by reducing the pressure inside the eye. The functional activities of cloned human β1 and β2 receptors are potently antagonistic to Levobetaxolol. Levobetaxolol(Ki = 16.4 nM) is more potent than dextrobetaxolol (Ki = 2.97 μM) at inhibiting isoproterenol-induced cAMP production in human non-pigmented ciliary epithelial cells.
| Targets |
β1-adrenergic receptor ( Ki = 0.76 nM ); β2-adrenergic receptor ( Ki = 32.6 nM )
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Levobetaxolol is applied topically to the eye but some does reach systemic circulaton with a Tmax of 3 h. Biological Half-Life The mean half life of levobetaxolol is 20 h. |
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| References | |||
| Additional Infomation |
Levobetaxolol Hydrochloride is the hydrochloride salt form of levobetaxolol, the S-isomer of the -selective beta-1 adrenergic receptor antagonist betaxolol with anti-glaucoma activity and devoid of intrinsic sympathomimetic activity. When applied topically in the eye, levobetaxolol reduces aqueous humor secretion and lowers the intraocular pressure (IOP).
See also: Levobetaxolol (has active moiety). Glaucoma is a chronic optic neuropathy in which retinal ganglion cells die over a number of years. The initiation of the disease and its progression may involve an ischaemic-like insult to the ganglion cell axons caused by an alteration in the quality of blood flow. Thus, to effectively treat glaucoma it may be necessary to counteract the ischaemic-like insult to the region of the optic nerve head. Studies on the isolated optic nerve suggest that substances that reduce the influx of sodium would be particularly effective neuroprotectants. Significantly, of the presently used antiglaucoma substances, only beta-blockers can reduce sodium influx into cells. Moreover, they also reduce the influx of calcium and this would be expected to benefit the survival of insulted neurones. Betaxolol is the most effective antiglaucoma drug at reducing sodium/calcium influx. Our electroretinographic data indicated that topical application of levobetaxolol to rats attenuated the effects of ischaemia/reperfusion injury. Timolol was also effective but to a lesser extent. Based on these data we conclude that beta-blockers may be able to blunt ganglion cell death in glaucoma, and that levobetaxolol may be a more effective neuroprotectant than timolol because of its greater capacity to block sodium and calcium influx.[2] |
| Molecular Formula |
C18H30CLNO3
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| Molecular Weight |
343.89
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| Exact Mass |
343.191
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| Elemental Analysis |
C, 62.87; H, 8.79; Cl, 10.31; N, 4.07; O, 13.96
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| CAS # |
116209-55-3
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| Related CAS # |
Betaxolol; 63659-18-7; Betaxolol hydrochloride; 63659-19-8
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| PubChem CID |
60656
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| Appearance |
White to off-white solid powder
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| Boiling Point |
448ºC at 760 mmHg
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| Flash Point |
224.7ºC
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| Vapour Pressure |
8.26E-09mmHg at 25°C
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| LogP |
3.586
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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 |
11
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| Heavy Atom Count |
23
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| Complexity |
286
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| Defined Atom Stereocenter Count |
1
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| SMILES |
Cl[H].O(C([H])([H])C([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])OC([H])([H])[C@]([H])(C([H])([H])N([H])C([H])(C([H])([H])[H])C([H])([H])[H])O[H])C([H])([H])C1([H])C([H])([H])C1([H])[H]
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| InChi Key |
CHDPSNLJFOQTRK-LMOVPXPDSA-N
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| InChi Code |
InChI=1S/C18H29NO3.ClH/c1-14(2)19-11-17(20)13-22-18-7-5-15(6-8-18)9-10-21-12-16-3-4-16;/h5-8,14,16-17,19-20H,3-4,9-13H2,1-2H3;1H/t17-;/m0./s1
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| Chemical Name |
(2S)-1-[4-[2-(cyclopropylmethoxy)ethyl]phenoxy]-3-(propan-2-ylamino)propan-2-ol;hydrochloride
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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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 (7.27 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 (7.27 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 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: 120 mg/mL (348.95 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9079 mL | 14.5395 mL | 29.0791 mL | |
| 5 mM | 0.5816 mL | 2.9079 mL | 5.8158 mL | |
| 10 mM | 0.2908 mL | 1.4540 mL | 2.9079 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 |
| NCT00061516 | Completed | Drug: BETAXON (levobetaxolol HCl) Drug: AZOPT (brinzolamide) |
Ocular Hypertension Glaucoma |
Alcon Research | January 2003 | Phase 3 |
| NCT02617459 | Completed | Drug: Levobetaxolol eye drops Drug: Betaxolol eye drops |
Primary Open-angle Glaucoma Ocular Hypertension |
Zhaoke (Guangzhou) Ophthalmology Pharmaceutical Ltd. |
January 4, 2019 | Phase 3 |
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