| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
| Targets |
β adrenergic receptor
Levosalbutamol tartrate targets the β₂-adrenergic receptor, acting as a relatively selective agonist. By binding to and activating these receptors on airway smooth muscle, it causes bronchodilation, relieving the symptoms of asthma and COPD. |
|---|---|
| ln Vitro |
In vitro, Levosalbutamol tartrate is a potent agonist of the β₂-adrenergic receptor. Its activity is due to the R-enantiomer, which is the pharmacologically active form of salbutamol. It causes relaxation of airway smooth muscle in vitro.
|
| ln Vivo |
In vivo, Levosalbutamol tartrate is an effective bronchodilator used clinically to treat asthma and COPD. It is administered via inhalation for rapid onset of action. Its use as the pure R-enantiomer is thought to reduce side effects compared to the racemic mixture.
|
| Enzyme Assay |
In vitro non-cell enzyme/receptor binding assays for Levosalbutamol tartrate involve measuring its binding affinity to the β₂-adrenergic receptor using radioligand binding studies. Membranes from cells expressing the receptor are incubated with the compound and a radiolabeled antagonist, and the Ki is determined.
|
| Cell Assay |
In vitro cell-based assays for Levosalbutamol tartrate use cell lines expressing the β₂-adrenergic receptor. The compound's ability to activate the receptor is measured by monitoring the accumulation of cyclic AMP (cAMP), a downstream second messenger. EC₅₀ values are calculated.
|
| Animal Protocol |
In vivo animal studies for Levosalbutamol tartrate employ models of bronchoconstriction, such as histamine- or methacholine-induced bronchospasm in guinea pigs or other rodents. The compound is administered by inhalation, and its ability to reverse bronchoconstriction is measured.
|
| ADME/Pharmacokinetics |
Levosalbutamol tartrate has a molecular weight of 628.71 g/mol and a molecular formula of C₃₀H₄₈N₂O₁₂. It is the tartrate salt of levosalbutamol. It is formulated as an inhalation solution for clinical use. Detailed pharmacokinetic parameters, such as absorption, distribution, metabolism, and excretion (ADME), are well characterized from its clinical use.
|
| Toxicity/Toxicokinetics |
Levosalbutamol tartrate has a well-established safety profile from its clinical use. Common side effects include tremor, tachycardia, and nervousness, which are typical of β₂-agonists. At high doses, it can cause hypokalemia and cardiac arrhythmias. Its use as the R-enantiomer is associated with a reduced incidence of side effects compared to the racemic mixture.
|
| References | |
| Additional Infomation |
Levosalbutamol tartrate (levalbuterol) is the R-enantiomer of salbutamol, a short-acting β₂-adrenergic receptor agonist used for the treatment of asthma and COPD. It is the pharmacologically active enantiomer, providing bronchodilation with potentially fewer side effects. It is clinically available as an inhalation solution.
|
| Molecular Formula |
C30H48N2O12
|
|---|---|
| Molecular Weight |
628.71
|
| CAS # |
661464-94-4
|
| Related CAS # |
Levalbuterol hydrochloride; 50293-90-8; Levalbuterol; 34391-04-3
|
| PubChem CID |
10349032
|
| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
12
|
| Hydrogen Bond Acceptor Count |
14
|
| Rotatable Bond Count |
13
|
| Heavy Atom Count |
44
|
| Complexity |
361
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
OC1=C(CO)C=C([C@@H](O)CNC(C)(C)C)C=C1.OC2=C(CO)C=C([C@@H](O)CNC(C)(C)C)C=C2.OC([C@H](O)[C@@H](O)C(O)=O)=O
|
| Synonyms |
Levalbuterol tartrate; Levosalbutamol tartrate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~159.1 mM)
Water: ~100 mg/mL |
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5906 mL | 7.9528 mL | 15.9056 mL | |
| 5 mM | 0.3181 mL | 1.5906 mL | 3.1811 mL | |
| 10 mM | 0.1591 mL | 0.7953 mL | 1.5906 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 |
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
