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| 5mg |
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| 10mg |
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| 25mg |
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Metipranolol is a potent non-selective beta blocker (β adrenergic receptor antagonist) used in eye drops to treat glaucoma. It breaks down quickly to produce desacetylmetipranolol.
| Targets |
β adrenergic receptor
|
|---|---|
| ln Vitro |
Metipranolol is applied topically to treat glaucoma and systemically to treat arterial hypertension[1].
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation Based on its physicochemical properties and ocular route of administration, metenolol eye drops are not expected to have any adverse effects on breastfed infants. Some guidelines indicate that the gel formulation is preferred over the solution formulation. To significantly reduce the amount of medication that enters breast milk after instillation, press your finger against the tear duct near the corner of your eye for at least 1 minute, then blot away any excess medication with absorbent paper. ◉ Effects on Breastfed Infants As of the revision date, no published information was found regarding metenolol. A study of breastfeeding mothers taking beta-blockers found a numerically increased number of adverse events, but this was not statistically significant. Although the infants' ages were matched to those in the control group, the ages of the affected infants were not specified. None of the mothers were taking metenolol. ◉ Effects on Lactation and Breast Milk As of the revision date, no published information was found regarding the effects of beta-blockers or metenolol during normal lactation. A study of six patients with hyperprolactinemia and galactorrhea found no change in serum prolactin levels after beta-adrenergic blockade with propranolol. |
| References |
| Molecular Formula |
C17H28CLNO4
|
|---|---|
| Molecular Weight |
345.86152
|
| Exact Mass |
345.171
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| Elemental Analysis |
C, 59.04; H, 8.16; Cl, 10.25; N, 4.05; O, 18.50
|
| CAS # |
36592-77-5
|
| Related CAS # |
22664-55-7 |
| PubChem CID |
656682
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| Appearance |
Solid powder
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| Boiling Point |
484.5ºC at 760 mmHg
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| Flash Point |
246.8ºC
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| LogP |
3.467
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
|
| Heavy Atom Count |
23
|
| Complexity |
348
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC1=C(OC(C)=O)C(C)=C(C)C(OCC(O)CNC(C)C)=C1.[H]Cl
|
| InChi Key |
BLWNYSZZZWQCKO-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H27NO4.ClH/c1-10(2)18-8-15(20)9-21-16-7-11(3)17(22-14(6)19)13(5)12(16)4;/h7,10,15,18,20H,8-9H2,1-6H3;1H
|
| Chemical Name |
[4-[2-hydroxy-3-(propan-2-ylamino)propoxy]-2,3,6-trimethylphenyl] acetate;hydrochloride
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| Synonyms |
Metipranolol hydrochloride; OptiPranolol; Metipranolol; Metipranolol HCl
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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. |
| 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) |
DMSO: ~100 mg/mL (~289.1 mM)
H2O: ≥ 100 mg/mL (~289.1 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.23 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 (7.23 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 (7.23 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: 100 mg/mL (289.13 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 | 2.8913 mL | 14.4567 mL | 28.9134 mL | |
| 5 mM | 0.5783 mL | 2.8913 mL | 5.7827 mL | |
| 10 mM | 0.2891 mL | 1.4457 mL | 2.8913 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.
Products are for research use only; We do not sell to patients
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