A β1-AR antagonist
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Betaxolol (hydrochloride)

Item No. 18625

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[4-[2-(cyclopropylmethoxy)ethyl]phenoxy]-3-[(1-methylethyl)amino]-2-propanol, monohydrochloride
CAS Number
63659-19-8
Synonyms
  • SL 75212
Molecular Formula
C18H29NO3 • HCl
Formula Weight
343.9
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 25 mg/mlEthanol: 25 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
223, 275, 281 nm
SMILES
OC(CNC(C)C)COC1=CC=C(CCOCC2CC2)C=C1.Cl
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
InChi Key
CHDPSNLJFOQTRK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    5 mg

    $41

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    10 mg

    $72

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    50 mg

    $127

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    100 mg

    $211

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    Product Description

    Betaxolol is an antagonist of the β1-adrenergic receptor (β1-AR; Ki = 23 nM).1 It is selective for the β1-AR over the β2-AR (Ki = 790 nM). Betaxolol is cytotoxic to 10.014 pRSV-T human corneal epithelial cells.2 It reduces intraocular pressure in cynomolgus monkeys with ocular hypertension induced by laser trabeculoplasty when administered at a dose of 150 µg/animal.3 Betaxolol also inhibits sodium influx induced by the neurotoxin veratridine in rat cortical synaptosomes (IC50 = 28.3 µM).4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wellstein, A., Palm, D., and Belz, G.G. Affinity and selectivity of β-adrenoceptor antagonists in vitro. J. Cardiovasc. Pharmacol. 8(Suppl. 11), S36-S40 (1986).

    2. Pozarowska, D., Pozarowski, P., and Darzynkiewicz, Z. Cytometric assessment of cytostatic and cytotoxic effects of topical glaucoma medications on human epithelial corneal line cells. Cytometry B Clin. Cytom. 78(2), 130-137 (2010).

    3. Sharif, N.A., Xu, S.X., Crider, J.Y., et al. Levobetaxolol (Betaxon™) and other β-adrenergic antagonists: Preclinical pharmacology, IOP-lowering activity and sites of action in human eyes. J. Ocul. Pharmacol. Ther. 17(4), 305-317 (2001).

    4. Chidlow, G., Melena, J., and Osborne, N.N. Betaxolol, a β1-adrenoceptor antagonist, reduces Na+ influx into cortical sunaptosomes by direct interaction with Na+ channels: Comparison with other β-adrenoceptor antagonists. Br. J. Pharmacol. 130(4), 759-766 (2000).