| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
| Targets |
Cimbuterol targets β-adrenergic receptors (β-ARs). As an agonist, it binds to and activates these G protein-coupled receptors, leading to the stimulation of adenylate cyclase and an increase in intracellular cyclic AMP (cAMP). This pathway mediates smooth muscle relaxation in the airways (bronchodilation), uterine relaxation (tocolysis), and anabolic effects in skeletal muscle.
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| ln Vitro |
In vitro, Cimbuterol acts as a β-adrenergic receptor agonist. Its activity is typically assessed by measuring its ability to stimulate cAMP accumulation in cells expressing β-ARs. It has been used as a standard for the detection of veterinary residues. Its potency and efficacy as a β-agonist can be determined and compared to reference agonists like isoproterenol or clenbuterol.
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| ln Vivo |
In vivo, Cimbuterol has been used illicitly to promote growth and improve feed efficiency in livestock. As a β-adrenergic agonist, it would be expected to produce bronchodilation, tocolysis, and anabolic effects. It has been used as a standard for the simultaneous detection of multiple veterinary residues in commercial animal meat by LC-MS/MS. It is not approved for human or veterinary use.
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| Enzyme Assay |
For non-cell-based receptor binding assays, Cimbuterol can be evaluated using membrane preparations from cells expressing human β2-adrenergic receptors. Radioligand binding displacement experiments are performed using a suitable radiolabeled antagonist such as [3H]-CGP-12177. Membrane homogenates are incubated with increasing concentrations of the test compound and a fixed concentration of the radioligand. Bound radioligand is separated from free by rapid filtration through glass fiber filters. Non-specific binding is determined in the presence of excess unlabeled propranolol. IC50 values are calculated from displacement curves using nonlinear regression analysis.
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| Cell Assay |
For in vitro cellular assays, cells expressing the human β2-adrenergic receptor (e.g., CHO or HEK293 cells) are cultured in appropriate media. For functional activity, cells are treated with various concentrations of Cimbuterol, and the accumulation of intracellular cAMP is measured using a competitive ELISA or HTRF-based detection kit. The EC50 for cAMP stimulation is calculated from dose-response curves. The compound's potency and efficacy as a β-agonist can be determined.
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| Animal Protocol |
For in vivo animal studies, Cimbuterol is not typically used for therapeutic research due to its illicit use in livestock. However, it may be used in analytical studies as a standard for residue detection. In such studies, the compound is administered to animals, and tissue samples are collected for analysis by LC-MS/MS. Dosing regimens and routes of administration vary depending on the specific study objectives.
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| ADME/Pharmacokinetics |
Cimbuterol has a molecular weight of 233.31 and a molecular formula of C13H19N3O. It is a solid with a purity of ≥95%. The compound is slightly soluble in dichloromethane and methanol. It should be stored at -20°C. It is for research use only and is not for human or veterinary use.
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| Toxicity/Toxicokinetics |
The toxicity profile of Cimbuterol has not been extensively reported. As a β-adrenergic agonist, potential adverse effects may include tachycardia, tremors, and cardiac arrhythmias at high doses. The compound has been used illicitly to promote growth in livestock, but its safety for human consumption has not been established. It is for research use only and is not for human or veterinary use.
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| References |
[1]. Analysis of 10 β-agonists in pork meat using automated dispersive pipette extraction and LC-MS/MS. J Chromatogr B Analyt Technol Biomed Life Sci. 2018 May 1;1084:64-68.
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| Additional Infomation |
Cimbuterol is a β-adrenergic receptor agonist. It has been used as a standard for the simultaneous detection of multiple veterinary residues in commercial animal meat by LC-MS/MS. It has also been used illicitly to promote growth and improve feed efficiency in livestock. It is available for research purposes only and is not for human or veterinary use.
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| Molecular Formula |
C13H19N3O
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|---|---|
| Molecular Weight |
233.31
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| Exact Mass |
233.153
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| CAS # |
54239-39-3
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| Related CAS # |
Cimbuterol-d9;1246819-04-4
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| PubChem CID |
3027547
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| Appearance |
White to off-white solid powder
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| Melting Point |
189-191°C
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| LogP |
2.534
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
17
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| Complexity |
289
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)(C)NCC(C1=CC(=C(C=C1)N)C#N)O
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| InChi Key |
YKKQAXQGZIBJFS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H19N3O/c1-13(2,3)16-8-12(17)9-4-5-11(15)10(6-9)7-14/h4-6,12,16-17H,8,15H2,1-3H3
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| Chemical Name |
2-amino-5-[2-(tert-butylamino)-1-hydroxyethyl]benzonitrile
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| Synonyms |
Cimbuterol; 54239-39-3; DTXSID30388626; RefChem:577140; DTXCID90339593;
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| 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 | 4.2861 mL | 21.4307 mL | 42.8614 mL | |
| 5 mM | 0.8572 mL | 4.2861 mL | 8.5723 mL | |
| 10 mM | 0.4286 mL | 2.1431 mL | 4.2861 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.
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