Betaxolol HCl

Catalog No.S1827 Batch:S182701

Technical Data

Formula

C₁₈H₂₉NO₃.HCl

Molecular Weight

343.89

CAS No.

63659-19-8

Solubility (25°C)*

In vitro

DMSO

69 mg/mL (200.64 mM)

Water

69 mg/mL (200.64 mM)

Ethanol

69 mg/mL (200.64 mM)

In vivo (Add solvents to the product individually and in order)

Clear solution

Saline

30.0mg/ml

Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Betaxolol (SL 75212) is a β₁ adrenergic receptor blocker with IC50 of 6 μM.

Targets

β1-adrenergic receptor ^[1]

6 μM

In vitro

Betaxolol is able to protect retinal neurones. ^[2] Betaxolol attenuates the NMDA-induced influx of ⁴⁵Ca²⁺ while β-adrenoreceptor agonists are ineffective. ^[3] The glutamate-induced release of LDH is almost completely prevented when betaxolol (10 μM) is included. ^[4] Betaxolol (100 μM) is very effective in preventing the hypoxia-induced release of LDH from cortical cultures. ^[5]

In vivo

When Betaxolol is injected i.p. into the rats before ischaemia and on the days of reperfusion the changes to the calretinin and ChAT immunoreactivities are reduced and the reduction of the b-wave is prevented. Inclusion of betaxolol partially prevents the changes caused by NMDA and lack of oxygen/glucose. ^[5]

Protocol (from reference)

Cell Assay:^{^[5]}	Cell lines Dissociated rat cortical cells Concentrations 100 μM Incubation Time 4 hours Method 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 consisting of transferrin (1 mg/mL), insulin (250 μg/mL) putrescine (600 μM), sodium selenite (0.3 μM), progesterone (0.2 μM) and estradiol (0.1 pM) for 7 days in an atmosphere of 5% CO₂/95% O₂ at 37 °C. The cultures are then transferred to a culture medium which lacks the hormonal supplemented medium. L-glutamate is added to the medium and incubated for a further 4 hours under normoxic conditions. Betaxolol are added to the cultures at the same time as L-glutamate. In other experiments the cultures are subjected to anoxic conditions, 95% N₂/5% CO₂, for 5 hours at 37 °C. Betaxolol is added prior to anoxia. Reoxygenation is then achieved by replacing the cells in normoxic conditions (95% O₂/5% CO₂) for 3 hours. Cellular injury is assessed by measuring lactate dehydrogenase (LDH) release into the cell culture supernatant after hypoxia/reoxygenation or glutamate exposure. LDH activity is assayed spectrophotometrically by following NADH metabolism for 2 minutes at 340 nm.
Animal Study:^{^[5]}	Animal Models Rat wiht ischaemia Dosages 2.5 mg/kg Administration Administered via i.p.

Cell Assay:^{^[5]}

Cell lines
Dissociated rat cortical cells
Concentrations
100 μM
Incubation Time
4 hours
Method
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 consisting of transferrin (1 mg/mL), insulin (250 μg/mL) putrescine (600 μM), sodium selenite (0.3 μM), progesterone (0.2 μM) and estradiol (0.1 pM) for 7 days in an atmosphere of 5% CO₂/95% O₂ at 37 °C. The cultures are then transferred to a culture medium which lacks the hormonal supplemented medium. L-glutamate is added to the medium and incubated for a further 4 hours under normoxic conditions. Betaxolol are added to the cultures at the same time as L-glutamate. In other experiments the cultures are subjected to anoxic conditions, 95% N₂/5% CO₂, for 5 hours at 37 °C. Betaxolol is added prior to anoxia. Reoxygenation is then achieved by replacing the cells in normoxic conditions (95% O₂/5% CO₂) for 3 hours. Cellular injury is assessed by measuring lactate dehydrogenase (LDH) release into the cell culture supernatant after hypoxia/reoxygenation or glutamate exposure. LDH activity is assayed spectrophotometrically by following NADH metabolism for 2 minutes at 340 nm.

Animal Study:^{^[5]}

Animal Models
Rat wiht ischaemia
Dosages
2.5 mg/kg
Administration
Administered via i.p.

References

Selleck's Betaxolol HCl has been cited by 1 publication

Box-Behnken response surface modeling assisted enantiomeric resolution of some racemic β-blockers using HPTLC and β-cyclodextrin as chiral mobile phase additive: Application to check the enantiomeric purity of betaxolol [ Chirality, 2018, 30(11):1195-1205]	PubMed: 30193408

Box-Behnken response surface modeling assisted enantiomeric resolution of some racemic β-blockers using HPTLC and β-cyclodextrin as chiral mobile phase additive: Application to check the enantiomeric purity of betaxolol [ Chirality, 2018, 30(11):1195-1205]

PubMed: 30193408

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.