| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Betaxolol HCl (Betoptima; Kerlone; Betoptic; Kerlon; SL-75212; ALO-1401-02; ALO140102), the hydrochloride salt of Betaxolol, is a potent beta-1/β1 adrenergic receptor antagonist with antihypertensive effects. It inhibits the beta-1/β1 adrenergic receptor with an IC50 of 6 μM. Currently, betaxolol is approved to treat glaucoma and hypertension.
| Targets |
β1-adrenergic receptor ( IC50 = 6 μM )
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| Cell Assay |
Dissociated cortical cells from 16–18-day-old fetal rats are grown in 35 mm dishes in DMEM supplemented with L-glutamine (4 mM), glucose (6 g/L), penicillin (100 U/mL), streptomycin (100 μg/mL), and 10% hormonal supplemented medium that contains sodium selenite (0.3 μM), progesterone (0.2 μM), putrescine (600 μM), transferrin (1 mg/mL), insulin (250 μg/mL), putrescine (600 μM), progesterone (0.2 μM), and estradiol (0.1 pM). After that, the cultures are moved to a culture medium without hormone supplements. After adding L-glutamate, the mixture is incubated under normoxic conditions for an additional 4 hours. L-glutamate and betaxolol are added to the cultures simultaneously. In anoxic conditions, 95% N2/5% CO2 for 5 hours at 37 °C, are applied to the cultures in other experiments. Anoxia occurs first, and then bexolol. Next, the cells are swapped out for normoxic ones (95% O2/5% CO2) for three hours in order to achieve reoxygenation. Measuring the release of lactate dehydrogenase (LDH) into the supernatant of cell cultures following hypoxia/reoxygenation or glutamate exposure is a useful method for evaluating cellular injury. By monitoring NADH metabolism for two minutes at 340 nm, LDH activity is measured spectrophotometrically.
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| References |
| Molecular Formula |
C18H30CLNO3
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| Molecular Weight |
343.89
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| Exact Mass |
343.19
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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 # |
63659-19-8
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| Related CAS # |
Betaxolol; 63659-18-7; Levobetaxolol hydrochloride; 116209-55-3; Betaxolol-d7 hydrochloride; 1219802-92-2
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| Appearance |
Solid powder
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| SMILES |
CC(C)NCC(COC1=CC=C(C=C1)CCOCC2CC2)O.Cl
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| InChi Key |
CHDPSNLJFOQTRK-UHFFFAOYSA-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
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| Chemical Name |
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 |
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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: ≥ 2.5 mg/mL (7.27 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: Saline: 30 mg/mL Solubility in Formulation 5: 130 mg/mL (378.03 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 |
| NCT01660620 | Completed | Drug: topical betaxolol Drug: Betaxolol |
Development of Side Effects From Betaxolol |
Smith-Kettlewell Eye Research Institute |
April 2011 | Phase 1 |
| NCT00061542 | Completed | Drug: BETOPTIC S (betaxolol HCl) Drug: Timolol Gel-forming Solution (TGFS) |
Glaucoma Ocular Hypertension |
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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