| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
| Targets |
Mapenterol hydrochloride targets the β2-adrenoceptor. 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, increased cardiac output, and enhanced lipolysis. It is a related drug of Clenbuterol.
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| ln Vitro |
In vitro, Mapenterol hydrochloride acts as a β2-adrenoceptor agonist. Its activity is typically assessed by measuring its ability to stimulate cAMP accumulation in cells expressing the β2-AR. As a structural analog of clenbuterol, it is presumed to share a similar pharmacological profile. Studies have investigated the interactions of mapenterol with serum albumins using multi-spectroscopy and molecular docking.
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| ln Vivo |
In vivo, Mapenterol hydrochloride can be used as a growth promoter in farm animals. As a β2-adrenoceptor agonist, it would be expected to produce bronchodilation, increased cardiac output, and anabolic effects. Its use as a growth promoter is related to its ability to promote muscle growth and improve feed efficiency. However, comprehensive in vivo pharmacological studies are limited.
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| Enzyme Assay |
For non-cell-based receptor binding assays, Mapenterol hydrochloride can be evaluated using membrane preparations from cells expressing the human β2-adrenergic receptor. 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 Mapenterol hydrochloride, 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 β2-agonist can be determined and compared to reference agonists like clenbuterol.
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| Animal Protocol |
For in vivo animal studies, Mapenterol hydrochloride is typically administered to farm animals via oral administration for growth promotion studies. In such studies, body weight gain, feed efficiency, and muscle mass are measured. Tissue samples may be collected for residue analysis to monitor the compound's distribution and elimination. Dosing regimens vary depending on the specific animal species and study objectives.
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| ADME/Pharmacokinetics |
Mapenterol hydrochloride has a molecular weight of 361.23 and a molecular formula of C14H21Cl2F3N2O. It has a melting point of 176-178°C (decomposition) and a LogP of 5.526. The compound is a white to off-white solid powder. It is soluble in DMSO and can be formulated for in vivo administration. The compound should be stored at -20°C for long-term stability.
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| Toxicity/Toxicokinetics |
The toxicity profile of Mapenterol hydrochloride has not been extensively reported. As a β2-adrenoceptor agonist, potential adverse effects may include tachycardia, tremors, and cardiac arrhythmias at high doses. The compound has been used as a growth promoter in farm animals, but its safety for human consumption has not been fully established. It is for research use only and is not intended for human consumption.
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| References |
[1]. Study on the interactions of mapenterol with serum albumins using multi-spectroscopy and molecular docking. Luminescence. 2016 Mar;31(2):372-379.
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| Additional Infomation |
Mapenterol hydrochloride belongs to the (trifluoromethyl)benzene class of compounds.
Mapenterol hydrochloride is a β2-adrenoceptor agonist and a related drug of Clenbuterol. It can be used as a growth promoter in farm animals. It is a member of (trifluoromethyl)benzenes. The compound has been studied for its interactions with serum albumins. It is available for research purposes only and is not for human use. |
| Molecular Formula |
C14H21CL2F3N2O
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|---|---|
| Molecular Weight |
361.23
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| Exact Mass |
360.098
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| CAS # |
54238-51-6
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| Related CAS # |
Mapenterol-d6 hydrochloride;1246816-02-3
Mapenterol HCl; 95656-68-1; 54238-51-6;
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| PubChem CID |
13355612
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| Appearance |
White to off-white solid powder
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| Melting Point |
176-178℃ (Decomposition)
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| LogP |
5.526
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
22
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| Complexity |
339
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)C(F)(F)F)O.Cl
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| InChi Key |
LWJSGOMCMMDPEN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H20ClF3N2O.ClH/c1-4-13(2,3)20-7-11(21)8-5-9(14(16,17)18)12(19)10(15)6-8;/h5-6,11,20-21H,4,7,19H2,1-3H3;1H
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| Chemical Name |
1-[4-amino-3-chloro-5-(trifluoromethyl)phenyl]-2-(2-methylbutan-2-ylamino)ethanol;hydrochloride
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| Synonyms |
Mapenterol HCl; 95656-68-1; Mapenterol hydrochloride; 54238-51-6; DTXSID60538091; RefChem:810599; DTXCID601784403; DTXSID10914886; RefChem:925315; DTXCID30981156;
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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 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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7683 mL | 13.8416 mL | 27.6832 mL | |
| 5 mM | 0.5537 mL | 2.7683 mL | 5.5366 mL | |
| 10 mM | 0.2768 mL | 1.3842 mL | 2.7683 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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