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Levobetaxolol HCl(AL-1577A)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Levobetaxolol HCl(AL-1577A)图片
CAS NO:116209-55-3
规格:≥98%
包装与价格:
包装价格(元)
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
2g电议
5g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)343.89
FormulaC18H29NO3.HCl
CAS No.116209-55-3 (HCl salt);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 69 mg/mL (200.6 mM)
Water: 69 mg/mL (200.6 mM)
Ethanol: 69 mg/mL (200.6 mM)
Other info
Chemical Name: (S)-1-(4-(2-(cyclopropylmethoxy)ethyl)phenoxy)-3-(isopropylamino)propan-2-ol hydrochloride
InChi Key: CHDPSNLJFOQTRK-LMOVPXPDSA-N
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/t17-;/m0./s1
SMILES Code: O[C@@H](CNC(C)C)COC1=CC=C(CCOCC2CC2)C=C1.[H]Cl
SynonymsAL 1577A; (S)-Betaxolol hydrochloride; AL 1577A; Levobetaxolol hydrochloride; AL-1577A; AL1577A; Betaxon
实验参考方法
In Vitro

In vitro activity: Levobetaxolol potently antagonizes functional activities at cloned human β1 and β2 receptors, and also at guinea pig atrial β1, tracheal β2 and rat colonic β3 receptors with IC50s of 33.2 nM, 2970 nM and 709 nM, respectively. Levobetaxolol (Ki = 16.4 nM) is more potent than dextrobetaxolol (Ki = 2.97 μM) at inhibiting isoproterenol-induced cAMP production in human non-pigmented ciliary epithelial cells. Levobetaxolol (topically applied) has been shown to reach the back of the eye in sufficient quantities to protect retinal ganglion cells from various types of insults. Levobetaxolol displaces [3H]-nitrendipine for L-type voltage-dependent calcium channel receptor with IC50 of 29.5 μM in rat cortex. Levobetaxolol reduces NMDA-stimulated 45Ca2+ influx by 47.3%. Levobetaxolol (topically applied) reduces the b-wave amplitude caused by ischaemia/reperfusion.

In VivoLevobetaxolol (150 mg/eye) is more potent than dextrobetaxolol, reducing intraocular pressure by 25.9% in conscious ocular hypertensive cynomolgus monkeys. Levobetaxolol (20 mg/kg) significant protects retinal function and results in significantly thicker the RPE and outer nuclear layer in a photic-induced retinopathy rat model. Levobetaxolol (20 mg/kg) results in a 10-fold up-regulation of bFGF and a two-fold up-regulation of CNTF mRNA levels, trophic factors that have been shown to inhibit retinal degeneration in a number of species.
Animal modelHypertensive cynomolgus monkeys
Formulation & Dosage20 mg/kg
ReferencesJ Ocul Pharmacol Ther. 2001 Aug;17(4):305-17; Exp Eye Res. 2002 Apr;74(4):445-53.