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    Betaxolol (SL75212)
    Betaxolol (SL75212)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1149
    CAS #: 63659-18-7Purity ≥98%

    Description: Betaxolol (Betoptima; Kerlone; Betoptic; Kerlon; SL-75212 HCl; ALO-140102) is a β1 adrenergic receptor antagonist/blocker with antihypertensive effects. It is used in the treatment of hypertension and glaucoma. Betaxolol inhibits  β1 adrenergic receptor with an IC50 of 6 μM.  

    References: Exp Eye Res. 2003 Apr;76(4):505-16; Exp Eye Res. 1999 Sep;69(3):331-42.

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    Molecular Weight (MW)307.43
    FormulaC18H29NO3
    CAS No.63659-18-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 62 mg/mL (201.7 mM)
    Water: <1 mg/mL
    Ethanol: 62 mg/mL (201.7 mM)  
    Other info

    Chemical Name: 2-Propanol, 1-(4-(2-(cyclopropylmethoxy)ethyl)phenoxy)-3-((1-methylethyl)amino)-

    InChi Key: NWIUTZDMDHAVTP-UHFFFAOYSA-N

    InChi Code: InChI=1S/C18H29NO3/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

    SMILES Code: OC(CNC(C)C)COC1=CC=C(CCOCC2CC2)C=C1

    SynonymsSL-75212 HCl; ALO 140102; ALO-1401-02; SL 75212 HCl; Betaxolol Hydrochloride; Betaxolol HCL; Betoptima; Kerlone; Betoptic; Kerlon; SL75212 HCl; ALO140102


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    In Vitro

    In vitro activity: Betaxolol is able to protect retinal neurons. Betaxolol attenuates the NMDA-induced influx of 45Ca2+ while β-adrenoreceptor agonists are ineffective. The glutamate-induced release of LDH is almost completely prevented when betaxolol (10 μM) is included. Betaxolol (100 μM) is very effective in preventing the hypoxia-induced release of LDH from cortical cultures.


    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 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.

    In VivoWhen 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. 
    Animal modelRat with ischemia model 
    Formulation & DosageDissolved in saline; 2.5 mg/kg; i.p. injection
    References

    Exp Eye Res. 2003 Apr;76(4):505-16; Exp Eye Res. 1999 Sep;69(3):331-42. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    BetaxololEffect of betaxolol on the DNA fragmentation of HCE cells. Int J Ophthalmol. 2014; 7(1): 14–21.
    Betaxolol
    Effect of betaxolol on cat corneas in vivo (n=4). Int J Ophthalmol. 2014; 7(1): 14–21.

     


    Betaxolol

    Effect of betaxolol on the histological structure of CCE cells in vivo. Int J Ophthalmol. 2014; 7(1): 14–21.


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