| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Target: Levosalbutamol targets the β2-adrenergic receptor, a G-protein coupled receptor located on bronchial smooth muscle cells. It acts as a selective sympathomimetic beta-2 adrenergic receptor agonist with bronchodilator activity. The R-enantiomer is responsible for the bronchodilatory activity of racemic albuterol. In therapeutic doses, it acts on beta-2 adrenoceptors of bronchial smooth muscle with minimal effect on myocardial beta-1 adrenoceptors.
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| ln Vitro |
Levalbuterol hydrochloride (10 μM; 24 hours) causes 11β-HSD1 mRNA expression in airway epithelial cells, but not 11β-HSD2 expression[1].
Levalbuterol (10 μM; 24 hours) hydrochloride decreases NF-κB activity induced by TNF-α and LPS significantly while increasing GRE activation in a manner dependent on 11β-HSD1 in a transformed mouse airway epithelial cell line[1]. In Vitro Activity: Levalbuterol hydrochloride (10 μM; 24 hours) causes 11β-HSD1 mRNA expression in airway epithelial cells but not 11β-HSD2 expression. It decreases NF-κB activity induced by TNF-α and LPS significantly while increasing GRE activation in a manner dependent on 11β-HSD1 in a transformed mouse airway epithelial cell line. The compound shows agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells with an EC50 of 145 nM for increasing IBMX-induced cAMP accumulation. |
| ln Vivo |
Levalbuterol hydrochloride (subcutaneous injection; 1 mg/kg; 14 days) dramatically reduces pulmonary inflammation in OVA mice, as evidenced by a drop in IgE and eosinophilia[2].
In Vivo Activity: Levalbuterol hydrochloride (subcutaneous injection; 1 mg/kg; 14 days) dramatically reduces pulmonary inflammation in ovalbumin (OVA)-sensitized mice, as evidenced by a drop in IgE and eosinophilia. (R)-salbutamol provides beneficial β2-agonist effects in experimental models of airways disease. When compared with racemic salbutamol, clinically comparable bronchodilation can be achieved with doses that substantially lessen beta-mediated side effects. |
| Enzyme Assay |
In Vitro Enzyme/Receptor Binding Protocol: β2-adrenergic receptor binding assays typically use membrane preparations from cells expressing the human β2-adrenoceptor. Radioligand binding with [3H]CGP-12177 or similar ligands is performed with varying concentrations of levosalbutamol to determine receptor affinity and binding kinetics. cAMP accumulation is measured using ELISA or radioimmunoassay to assess receptor activation. The compound's agonist activity is characterized by EC50 determination for cAMP accumulation.
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| Cell Assay |
Cell Line: Murine Club (MTCC) cells
Concentration: 10 μM Incubation Time: 24 hours Result: Increased 11β-HSD1 mRNA expression selectively. In Vitro Cell-Based Assay Protocol: Murine Club (MTCC) cells are treated with levalbuterol hydrochloride at 10 μM for 24 hours. 11β-HSD1 and 11β-HSD2 mRNA expression is measured by qPCR. NF-κB activity and GRE activation are assessed using reporter gene assays. HEK293T cells expressing recombinant human beta2 adrenoceptor are used to measure cAMP accumulation in response to compound treatment. Cell viability is monitored to ensure compound concentrations are not cytotoxic. |
| Animal Protocol |
C57BL/6 female mice with a pulmonary allergic model
1 mg/kg Subcutaneous injection; 1 mg/kg; 14 days In Vivo Animal Assay Protocol: C57BL/6 female mice with a pulmonary allergic model (OVA-sensitized) are used. Levalbuterol hydrochloride is administered via subcutaneous injection at 1 mg/kg for 14 days. Pulmonary inflammation is assessed by measuring IgE levels and eosinophilia. Bronchoalveolar lavage fluid is collected for cell count and cytokine analysis. Lung tissue is harvested for histopathological examination. |
| ADME/Pharmacokinetics |
Pharmacokinetics: Levosalbutamol is rapidly absorbed after inhalation with onset of action within minutes. It has a short duration of action typical of short-acting β2-agonists. The compound undergoes hepatic metabolism and is excreted primarily in urine. Detailed PK parameters including half-life, Cmax, and bioavailability have been characterized in clinical pharmacology studies. The R-enantiomer has a more favorable pharmacokinetic profile compared to the racemic mixture due to enantioselective disposition.
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| Toxicity/Toxicokinetics |
Toxicity: Levosalbutamol HCl has an established safety profile from extensive clinical use. Common adverse effects include tremor, tachycardia, and headache. The R-enantiomer has a more favorable safety profile compared to racemic albuterol with reduced cardiac effects because the (S)-enantiomer is associated with potential negative effects. At therapeutic doses, it has minimal effect on myocardial beta-1 adrenoceptors. The compound is FDA-approved for clinical use.
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| References | |
| Additional Infomation |
Levosalbutamol hydrochloride is the hydrochloride form of levosalbutamol, a relatively selective sympathomimetic β2-adrenergic receptor agonist with bronchodilatory effects. Levosalbutamol hydrochloride binds to β2-adrenergic receptors in bronchial smooth muscle, activating intracellular adenylate cyclase, thereby increasing the production of cyclic adenosine monophosphate (cAMP). Elevated cAMP levels activate protein kinase A, which inhibits myosin phosphorylation and reduces intracellular calcium ion concentration, ultimately leading to bronchial smooth muscle relaxation. Increased cAMP concentrations also inhibit the release of inflammatory mediators from mast cells.
The R-isomer of salbutamol. See also: Levosalbutamol (with active moiety). Additional Information: Levosalbutamol HCl has CAS number 50293-90-8, molecular formula C13H22ClNO3, and molecular weight 275.77. It is also known as levalbuterol HCl, Xopenex, (R)-albuterol, and R-albuterol. The compound is a relatively selective sympathomimetic beta-2 adrenergic receptor agonist with bronchodilator activity. It binds to beta-2 adrenergic receptors in bronchial smooth muscle and activates intracellular adenyl cyclase, increasing cAMP production, which leads to protein kinase A activation, inhibition of myosin phosphorylation, lowered intracellular calcium, and bronchial smooth muscle relaxation. Increased cAMP also inhibits release of inflammatory mediators from mast cells. FDA-approved for asthma and COPD. |
| Molecular Formula |
C13H22CLNO3
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| Molecular Weight |
275.77
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| Exact Mass |
275.128
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| Elemental Analysis |
C, 56.62; H, 8.04; Cl, 12.85; N, 5.08; O, 17.40
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| CAS # |
50293-90-8
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| Related CAS # |
Levalbuterol tartrate; 661464-94-4; Levalbuterol; 34391-04-3; 50293-90-8(HCl)
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| PubChem CID |
123601
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| Appearance |
White to off-white solid powder
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| Boiling Point |
433.5ºC at 760 mmHg
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| Melting Point |
169-171ºC
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| LogP |
2.498
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
18
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| Complexity |
227
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(C)(C)NC[C@@H](C1=CC(=C(C=C1)O)CO)O.Cl
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| InChi Key |
OWNWYCOLFIFTLK-YDALLXLXSA-N
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| InChi Code |
InChI=1S/C13H21NO3.ClH/c1-13(2,3)14-7-12(17)9-4-5-11(16)10(6-9)8-15;/h4-6,12,14-17H,7-8H2,1-3H3;1H/t12-;/m0./s1
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| Chemical Name |
4-[(1R)-2-(tert-butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)phenol;hydrochloride
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| Synonyms |
Levalbuterol HCl; Levosalbutamol HCl; Xopenex; (R)-albuterol; R-albuterol; R albuterol
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: ~100 mg/mL (~362.6 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (362.62 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6262 mL | 18.1311 mL | 36.2621 mL | |
| 5 mM | 0.7252 mL | 3.6262 mL | 7.2524 mL | |
| 10 mM | 0.3626 mL | 1.8131 mL | 3.6262 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00665600 | Completed | Drug: Levalbuterol HCl Drug: Albuterol Sulfate Drug: Placebo |
Chronic Obstructive Pulmonary Disease (COPD) |
Sumitomo Pharma America, Inc. | February 2002 | Phase 3 |
| NCT00667797 | Completed | Drug: levalbuterol HCl Drug: albuterol Sulfate |
Asthma COPD |
Sumitomo Pharma America, Inc. | March 2003 | Phase 4 |
| NCT00667407 | Recruiting | Drug: Levalbuterol 1.25 mg Drug: Racemic Albuterol Sulfate |
Asthma | Sumitomo Pharma America, Inc. | November 2000 | Phase 3 |
| NCT01076322 | Not yet recruiting | Drug: Meptin® Swinghaler Drug: Ventolin® MDI |
Asthma | Taiwan Otsuka Pharm. Co., Ltd | March 2009 | Phase 3 |
| NCT00583947 | Not yet recruiting | Drug: arformoterol Drug: levalbuterol |
Asthma | Sumitomo Pharma America, Inc. | January 2008 | Phase 2 |
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