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| Targets |
Procaterol hydrochloride hemihydrate targets the β2-adrenergic receptor. 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 cAMP. This pathway mediates smooth muscle relaxation in the airways, resulting in bronchodilation. The compound's β2-selectivity mediates its bronchodilatory effects with minimal cardiac side effects.
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| ln Vitro |
In human tracheal epithelial cells, procaterol hydrochloride hemihydrate (0.1 μM, 24-72 hours) suppresses rhinovirus infection [4]. In BEAS-2B cells, procaterol hydrochloride hemihydrate (0–1 μg/mL, 24/48 h) suppresses eosinophil chemotactic activity mediated by TNF-α and IL-1β [5]. Procaterol hydrochloride hemihydrate (25–200 nM, 20 h) guards against oxidative damage caused by H2O2 in 16HBE cells [6].
In vitro, Procaterol hydrochloride hemihydrate 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 or by evaluating its relaxing effects on isolated tracheal smooth muscle preparations. The compound's potency and efficacy as a β2-agonist can be determined and compared to reference agonists like salbutamol or isoproterenol. |
| ln Vivo |
In the airways of allergic, inflamed guinea pigs, procaterol hydrochloride hemihydrate (1, 3 or 10 μg/mL) suppresses histamine-induced airflow blockage and microvascular leakage[2]. In conscious guinea pigs, procaterol hydrochloride hemihydrate (0.1 mg/kg, ip) totally removes Mch-induced cough[3].
In vivo, Procaterol hydrochloride hemihydrate induces a strong bronchodilatory effect and is used in the treatment of bronchial asthma. It is a short-acting β2-agonist that provides rapid relief of bronchoconstriction. It has been studied for its function in patients with stable COPD treated with long-acting bronchodilators. The compound is orally active, making it suitable for oral administration in research settings. |
| Enzyme Assay |
For non-cell-based receptor binding assays, Procaterol hydrochloride hemihydrate 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 at room temperature for 60-90 minutes. 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 Procaterol hydrochloride hemihydrate, 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. For smooth muscle relaxation assays, isolated tracheal rings are pre-contracted and treated with the compound, and relaxation is measured isometrically.
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| Animal Protocol |
Animal/Disease Models: Allergic inflammatory guinea-pig model[2]
Doses: 1, 3 or 10 μg/mL Route of Administration: Inhaled administration Experimental Results: Inhibited histamine-induced airflow obstruction and microvascular leakage. For in vivo animal studies, Procaterol hydrochloride hemihydrate can be administered to rodents via oral gavage. In models of asthma or COPD, airway resistance and lung function parameters are measured following compound administration. In models of bronchoconstriction, the compound's ability to reverse induced bronchospasm is assessed. Dosing regimens vary depending on the specific model and desired exposure levels. Blood and tissue samples may be collected for pharmacokinetic analysis. |
| ADME/Pharmacokinetics |
Procaterol hydrochloride hemihydrate has a molecular formula of C16H25ClN2O4 and a molecular weight of 344.83. It is an orally active β2-adrenergic receptor agonist. The compound is supplied as a hydrochloride hemihydrate salt. It is for research use only and is not intended for human consumption.
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| Toxicity/Toxicokinetics |
The toxicity profile of Procaterol hydrochloride hemihydrate includes potential adverse effects associated with β2-agonists, including tachycardia, tremors, and hypokalemia at high doses. The compound is for research use only and is not intended for human consumption. Standard toxicological evaluation would include acute and repeated-dose toxicity studies, as well as assessment of cardiovascular and respiratory function.
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| References |
[1]. Tukiainen H, et al. Comparison between oral procaterol and salbutamol in patients with bronchial asthma. Curr Med Res Opin. 1988;11(4):236-41.
[2]. Mirza ZN, et al. Inhaled procaterol inhibits histamine-induced airflow obstruction and microvascular leakage in guinea-pig airways with allergic inflammation. Clin Exp Allergy. 1998 May;28(5):644-52. [3]. Ohkura N, et al. Bronchoconstriction-triggered cough in conscious guinea pigs. Exp Lung Res. 2009 May;35(4):296-306. [4]. Yamaya M, et al. Procaterol inhibits rhinovirus infection in primary cultures of human tracheal epithelial cells. Eur J Pharmacol. 2011 Jan 10;650(1):431-44. [5]. Koyama S, et al. Procaterol inhibits IL-1beta- and TNF-alpha-mediated epithelial cell eosinophil chemotactic activity. Eur Respir J. 1999 Oct;14(4):767-75. [6]. Deng Z, et al. Procaterol but not dexamethasone protects 16HBE cells from H₂O₂-induced oxidative stress. J Pharmacol Sci. 2014;125(1):39-50. |
| Additional Infomation |
Procaterol hydrochloride is an organic molecular entity. It is a long-acting β2-adrenergic receptor agonist. See also: Procaterol hydrochloride (note moved to).
Procaterol hydrochloride hemihydrate (CAS 81262-93-3) is an orally active β2-adrenergic receptor agonist. It induces a strong bronchodilatory effect and is used in the treatment of bronchial asthma. It is a short-acting β2-agonist used in respiratory research. It is available for research purposes only. |
| Molecular Formula |
C16H23CLN2O3.1/2H2O
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|---|---|
| Molecular Weight |
335.82
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| Exact Mass |
326.139
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| CAS # |
81262-93-3
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| Related CAS # |
Procaterol hydrochloride;62929-91-3;(Rac)-Procaterol hydrochloride;59828-07-8
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| PubChem CID |
656601
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| Appearance |
White to off-white solid powder
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| Boiling Point |
559.1ºC at 760 mmHg
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| Flash Point |
291.9ºC
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| LogP |
3.236
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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 |
22
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| Complexity |
397
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[C@@H](C1C=CC(O)=C2NC(C=CC=12)=O)(O)[C@@H](CC)NC(C)C.Cl.O
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| InChi Key |
AEQDBKHAAWUCMT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H22N2O3.ClH/c1-4-12(17-9(2)3)16(21)11-5-7-13(19)15-10(11)6-8-14(20)18-15;/h5-9,12,16-17,19,21H,4H2,1-3H3,(H,18,20);1H
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| Chemical Name |
8-hydroxy-5-[1-hydroxy-2-(propan-2-ylamino)butyl]-1H-quinolin-2-one;hydrochloride
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| Synonyms |
procaterol hydrochloride hemihydrate; Procaterol HCl hemihydrate; 62929-91-3; 4VD1BRT7T8; Pro-Air; Lontermin;
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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: 25 mg/mL (74.44 mM)
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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 | 2.9778 mL | 14.8889 mL | 29.7779 mL | |
| 5 mM | 0.5956 mL | 2.9778 mL | 5.9556 mL | |
| 10 mM | 0.2978 mL | 1.4889 mL | 2.9778 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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