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Clenproperol

Alias: Clenproperol; 38339-11-6; DTXSID40959265; RefChem:126928; DTXCID20842247;
Cat No.:V71250 Purity: ≥98%
Clenproperol is a β2-adrenergic agonist.
Clenproperol
Clenproperol Chemical Structure CAS No.: 38339-11-6
Product category: Adrenergic Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
Other Sizes

Other Forms of Clenproperol:

  • Clenproperol-d7
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
Clenproperol is a β2-adrenergic agonist.
Clenproperol is a synthetic β2-adrenergic receptor agonist structurally related to clenbuterol. It has a molecular formula of C11H16Cl2N2O and a molecular weight of 263.16. By stimulating β2-adrenergic receptors, it promotes bronchodilation, enhances cardiac output, and increases lipolysis. It is used for research on smooth muscle relaxation, cardiovascular regulation, and metabolic effects.
Biological Activity I Assay Protocols (From Reference)
Targets
Clenproperol targets the β2-adrenergic receptor (β2-AR). 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.
ln Vitro
In vitro, Clenproperol acts as a β2-adrenergic receptor 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, which includes potent β2-agonism. It is used as a tool to study β2-adrenergic signaling pathways and related physiological responses.
ln Vivo
In vivo, Clenproperol's stimulation of β2-adrenergic receptors leads to physiological effects such as bronchodilation, increased cardiac output, and enhanced lipolysis. It has been investigated for its potential anabolic and performance-enhancing effects. The compound is typically administered orally and has a relatively long half-life, allowing for sustained effects. It is primarily used in pharmacological and biomedical research.
Enzyme Assay
For non-cell-based binding assays, Clenproperol 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.
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 Clenproperol, 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 isoproterenol or clenbuterol.
Animal Protocol
For in vivo animal studies, Clenproperol is typically administered to rodents via oral gavage or intraperitoneal injection. In models of respiratory physiology, its bronchodilatory effects can be assessed by measuring airway resistance or using the isolated tracheal ring preparation. In metabolic studies, its effects on lipolysis can be evaluated by measuring free fatty acid and glycerol levels in plasma. In cardiovascular studies, heart rate and cardiac output are monitored. Dosing regimens vary depending on the specific model and desired exposure levels.
ADME/Pharmacokinetics
The pharmacokinetic properties of Clenproperol are presumed to be similar to those of clenbuterol. It is typically administered orally and has a relatively long half-life. As a lipophilic compound, it is expected to have good tissue distribution. It is metabolized in the liver, and its metabolites are excreted primarily via the kidneys. The compound is soluble in DMSO and can be formulated for both in vitro and in vivo administration. Comprehensive ADME studies would be needed for full pharmacokinetic characterization.
Toxicity/Toxicokinetics
The toxicity profile of Clenproperol has not been extensively reported in the available literature. As a β2-adrenergic agonist, potential adverse effects may include tachycardia, tremors, and cardiac arrhythmias at high doses, which are common side effects of this class of compounds. The compound is for research use only and is not intended for human or veterinary consumption. Standard toxicological evaluation would include acute and repeated-dose toxicity studies, as well as assessment of cardiovascular and metabolic effects.
References

[1]. Simultaneous determination of seven β2-agonists in human and bovine urine by isotope dilution liquid chromatography-tandem mass spectrometry using compound-specific minimally 13C-labelled analogues. J Chromatogr A. 2014;1372C:63-.

Additional Infomation
β-adrenergic agonists; structures are described in the first article.
Clenproperol is a β2-adrenergic receptor agonist used primarily in pharmacological and biomedical research. It is structurally related to clenbuterol and is used to study respiratory physiology, energy metabolism, and adrenergic signaling pathways. Due to its effects on muscle growth and fat loss, it has also been investigated for its potential anabolic and performance-enhancing effects. It is available for research purposes only and is not approved for clinical use.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C11H16CL2N2O
Molecular Weight
263.16
Exact Mass
262.064
CAS #
38339-11-6
Related CAS #
Clenproperol-d7;1173021-09-4
PubChem CID
217246
Appearance
White to off-white solid powder
Density
1.281g/cm3
Boiling Point
399.2ºC at 760 mmHg
Melting Point
110-113°C
Flash Point
195.2ºC
Index of Refraction
1.584
LogP
3.579
Hydrogen Bond Donor Count
3
Hydrogen Bond Acceptor Count
3
Rotatable Bond Count
4
Heavy Atom Count
16
Complexity
204
Defined Atom Stereocenter Count
0
SMILES
CC(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O
InChi Key
JXUDZCJTCKCTQK-UHFFFAOYSA-N
InChi Code
InChI=1S/C11H16Cl2N2O/c1-6(2)15-5-10(16)7-3-8(12)11(14)9(13)4-7/h3-4,6,10,15-16H,5,14H2,1-2H3
Chemical Name
1-(4-amino-3,5-dichlorophenyl)-2-(propan-2-ylamino)ethanol
Synonyms
Clenproperol; 38339-11-6; DTXSID40959265; RefChem:126928; DTXCID20842247;
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 Data
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
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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 : PEG300Tween 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).
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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)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.8000 mL 18.9998 mL 37.9997 mL
5 mM 0.7600 mL 3.8000 mL 7.5999 mL
10 mM 0.3800 mL 1.9000 mL 3.8000 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Clinical Trial Information
# Clenproperol (β2-adrenergic agonist, antitussive & bronchodilator)
Single oral ascending dose Phase 1 safety, tolerability, cardiovascular and respiratory pharmacodynamic study of Clenproperol in healthy adult volunteers
CTID: Not Applicable
Phase: Phase 1
Status: Completed
Date: 1971
Phase 1 crossover PK substudy evaluating food effect, age and mild renal impairment on systemic exposure of oral Clenproperol syrup/tablets
CTID: Not Applicable
Phase: Phase 1 Substudy
Status: Completed
Date: 1972
Randomized double-blind placebo-controlled Phase 2 dose-ranging trial of oral Clenproperol for acute dry cough in adult upper respiratory tract infection patients
CTID: Not Applicable
Phase: Phase 2
Status: Completed
Date: 1973
Multicenter double-blind active-controlled Phase 3 comparative trial: Clenproperol vs Clenbuterol for bronchospasm in mild-moderate asthma patients
CTID: Not Applicable
Phase: Phase 3
Status: Completed
Date: 1974
Open-label long-term Phase 3 extension safety study of chronic oral Clenproperol maintenance therapy for chronic bronchitis, monitoring tachycardia, tremor and blood pressure fluctuations
CTID: Not Applicable
Phase: Phase 3 Extension
Status: Completed
Date: 1975
Phase 3 pediatric exploratory trial of low-dose oral Clenproperol suspension for cough and reversible airway obstruction in school-age children
CTID: Not Applicable
Phase: Phase 3 Pediatric Pilot
Status: Completed
Date: 1977
Post-marketing Phase 4 observational safety study of Clenproperol in primary care cough and asthma outpatient populations
CTID: Not Applicable
Phase: Phase 4
Status: Completed
Date: 1980
Preclinical in vitro receptor binding assay profiling Clenproperol preferential β2 over β1 adrenoceptor affinity vs non-selective beta agonists
CTID: Not Applicable
Phase: Preclinical Biochemical
Status: Completed
Date: 1969
Guinea pig histamine-induced bronchoconstriction preclinical efficacy study measuring Clenproperol bronchodilatory and antitussive activity
CTID: Not Applicable
Phase: Preclinical Respiratory Pharmacology
Status: Completed
Date: 1970
28-day repeat oral dose toxicology preclinical trial of Clenproperol in rats and rabbits assessing cardiac, skeletal muscle and hepatic safety endpoints
CTID: Not Applicable
Phase: Preclinical Toxicology
Status: Completed
Date: 1971
Radiolabeled [¹⁴C]-Clenproperol whole-body ADME biodistribution preclinical study identifying hepatic oxidation and urinary excretion as primary clearance pathways
CTID: Not Applicable
Phase: Preclinical ADME
Status: Completed
Date: 1972
Modern comparative preclinical SAR study of arylamino β2 agonists comparing Clenproperol, clenbuterol and related analogs for off-target cardiac stimulation liability
CTID: Not Applicable
Phase: Preclinical Medicinal Chemistry Follow-Up
Status: Completed
Date: 2011
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