Levobetaxolol
Levobetaxolol is a potent and high affinity β-adrenergic antagonist with IC50 values of 33.2, 2970, 709 nM for guinea pig atrial β1, tracheal β2 and rat colonic β3 receptors, respectively. Levobetaxolol reduces IOP (intraocular pressure). Levobetaxolol exhibits a micromolar affinity for L-type Ca21-channels. Levobetaxolol decreases the effects of ischaemia/reperfusion injury in rats. Levobetaxolol has the potential for the research of glaucoma.
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- CAS No.: 93221-48-8
- Formule: C18H29NO3
- Masse moléculaire:307.43
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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β1 adrenoceptor 33.2 nM (IC50) |
β2 adrenoceptor 2970 nM (IC50) |
β3 adrenoceptor 709 nM (IC50) |
Levobetaxolol shows a higher affinity at cloned human β1 and β2 receptor with Ki values of 0.76, 32.6 nM, respectively[1].
Levobetaxolol inhibits functional activities in cells expressing human recombinant β1 and β2 receptors with Kb values of 6, 39 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 93221-48-8
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Masse moléculaire 307.43
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Formule C18H29NO3
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SMILES
O[C@H](COC1=CC=C(C=C1)CCOCC2CC2)CNC(C)C
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Synonyms
(S)-Betaxolol
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Sharif NA, et al. Levobetaxolol (Betaxon) and other beta-adrenergic antagonists: preclinical pharmacology, IOP-lowering activity and sites of action in human eyes. J Ocul Pharmacol Ther. 2001 Aug;17(4):305-17. [Content Brief]
[2]. Osborne NN, et al. Effectiveness of levobetaxolol and timolol at blunting retinal ischaemia is related to their calcium and sodium blocking activities: relevance to glaucoma. Brain Res Bull. 2004 Feb 15;62(6):525-8. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Levobetaxolol Related Classifications
HY-121166 Related Classifications
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