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| 50mg |
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| Targets |
Metaproterenol hemisulfate is a direct-acting sympathomimetic amine that acts as a beta-adrenergic agonist, specifically binding to the beta-2 adrenergic receptor (ADRB2). It has an IC50 of 68 nM for the β2AR. Upon binding to the receptor, it activates adenylyl cyclase, leading to increased production of cyclic adenosine monophosphate (cAMP). This triggers a range of downstream signaling pathways that result in bronchodilation and smooth muscle relaxation. The compound also has anti-inflammatory activity. Its therapeutic effects are mediated through β2AR activation in the airways.
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| ln Vitro |
Treatment of THP-1 cells and bone marrow macrophages with metaproterenol (10 μM; 74 hours) improves high glucose-induced β-arrestin2 and its association with IκBα [1]. Treatment with isoproterenol (10 μM; 74 hours; THP-1 cells and bone marrow macrophages) causes a significant downregulation of NF-κB in response to high glucose [1].
In vitro, Metaproterenol hemisulfate is a β2-adrenergic receptor agonist with an IC50 of 68 nM. It activates adenylyl cyclase in cells expressing the β2AR, leading to increased cAMP production. The compound has been used to study its effects on adenylyl cyclase stimulation in red blood cell deformability. Its in vitro activity is characterized by potent agonism at the β2AR and downstream cAMP signaling. Metaproterenol hemisulfate also exhibits anti-inflammatory activity in various in vitro assays. |
| ln Vivo |
Metaproterenol treatment for 12 weeks reduced monocyte activation and pro-inflammatory and pro-fibrotic responses in the kidney and heart of Zucker diabetic adipose rats. Consequently, metaproterenol may protect against renal and cardiovascular problems associated with diabetes [1].
In vivo, Metaproterenol hemisulfate shows bronchodilator activity and shows therapeutic effects against bronchitis, asthma, and emphysema. It is used in the treatment of asthma and bronchial spasm. The compound is a direct-acting sympathomimetic drug that acts as a β2AR agonist. Its in vivo efficacy is attributed to its ability to relax bronchial smooth muscle and improve airflow. The compound is administered via inhalation for the treatment of respiratory conditions. Its bronchodilator effects are rapid and well-characterized. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Metaproterenol hemisulfate typically involve measuring its binding affinity to the beta-2 adrenergic receptor (ADRB2). Radioligand binding assays using membrane preparations expressing the β2AR are performed to determine the IC50, which is 68 nM. These assays confirm the compound's mechanism of action as a β2AR agonist. The compound's ability to activate adenylyl cyclase and increase cAMP production can also be assessed using enzymatic assays.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: THP-1 cells and bone marrow macrophages Tested Concentrations: 10 μM Incubation Duration: 74 hrs (hours) Experimental Results: Enhanced β-arrestin2 and its interaction with IκBα. RT-PCR[1] Cell Types: THP-1 cells and bone marrow macrophages Tested Concentrations: 10 μM Incubation Duration: 74 hrs (hours) Experimental Results: Result in downregulation of NF-κB. In vitro cellular assays for Metaproterenol hemisulfate typically involve treating cells expressing the β2AR with the compound and measuring downstream signaling events such as cAMP production. The compound activates adenylyl cyclase and increases cAMP levels in a concentration-dependent manner. Its IC50 of 68 nM for the β2AR is confirmed in these cellular assays. These cell-based studies demonstrate the compound's functional agonism at the β2AR and its ability to activate downstream signaling pathways. |
| Animal Protocol |
In vivo animal models for Metaproterenol hemisulfate typically involve models of bronchoconstriction or asthma to evaluate its bronchodilator efficacy. The compound is administered by inhalation or other routes, and bronchial resistance or airflow is measured. It shows bronchodilator activity and therapeutic effects against bronchitis and asthma. Doses and administration routes are optimized based on the specific model and experimental endpoints. These studies provide evidence for the compound's in vivo efficacy as a bronchodilator.
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| ADME/Pharmacokinetics |
Metaproterenol hemisulfate is a direct-acting sympathomimetic drug with favorable pharmacokinetic properties for inhalation administration. It is rapidly absorbed through the airways and achieves therapeutic concentrations in the lungs. The compound is metabolized in the liver and excreted primarily in the urine. Its half-life supports frequent dosing for the management of acute bronchospasm. The compound's pharmacokinetic profile is well-characterized from its clinical use as a bronchodilator.
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| Toxicity/Toxicokinetics |
Metaproterenol hemisulfate is a well-tolerated medication with a favorable safety profile. Common adverse effects include tachycardia, tremors, and nervousness, which are related to its sympathomimetic activity. The compound should be used with caution in patients with cardiovascular disease, hypertension, or hyperthyroidism. Its safety profile is well-established from clinical use. Metaproterenol hemisulfate is for research use only and is not approved for human therapeutic use in many applications.
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| References |
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| Additional Infomation |
Metaproterenol sulfate is the sulfate form of Metaproterenol, a short-acting, selective sympathomimetic β-receptor agonist with bronchodilatory effects. Metaproterenol sulfate binds to β2-adrenergic receptors in bronchial smooth muscle, stimulating intracellular adenylate cyclase, thereby increasing the production of cyclic adenosine monophosphate (cAMP). Elevated cAMP levels lead to bronchial smooth muscle relaxation, improved mucus clearance, and reduced release of inflammatory mediators, particularly those from mast cells. It is a β2-adrenergic agonist used to treat asthma and bronchospasm.
Metaproterenol Hemisulfate (CAS# 5874-97-5), also known as Orciprenaline hemisulfate, is a direct-acting sympathomimetic drug and β2-adrenergic receptor (β2AR) agonist with an IC50 of 68 nM. It has anti-inflammatory activity and shows bronchodilator activity, with therapeutic effects against bronchitis, asthma, and emphysema. The compound acts by binding to the beta-2 adrenergic receptor (ADRB2), leading to increased cAMP production. It is used in the treatment of asthma and bronchial spasm. The compound is for research use only and is not approved for human therapeutic use in many applications. |
| Molecular Formula |
2[C11H18NO3+].O4S-2
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| Molecular Weight |
520.59364
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| Exact Mass |
520.209
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| CAS # |
5874-97-5
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| Related CAS # |
Metaproterenol;586-06-1;Metaproterenol-d7 hemisulfate
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| PubChem CID |
441333
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.199g/cm3
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| Boiling Point |
417.5ºC at 760mmHg
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| Melting Point |
202-203°
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| Flash Point |
179.7ºC
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| LogP |
3.468
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
35
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| Complexity |
258
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MKFFGUZYVNDHIH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/2C11H17NO3.H2O4S/c2*1-7(2)12-6-11(15)8-3-9(13)5-10(14)4-8;1-5(2,3)4/h2*3-5,7,11-15H,6H2,1-2H3;(H2,1,2,3,4)
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| Chemical Name |
5-[1-hydroxy-2-(propan-2-ylamino)ethyl]benzene-1,3-diol;sulfuric acid
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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) |
DMSO : ~62.5 mg/mL (~240.11 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.99 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9209 mL | 9.6045 mL | 19.2090 mL | |
| 5 mM | 0.3842 mL | 1.9209 mL | 3.8418 mL | |
| 10 mM | 0.1921 mL | 0.9604 mL | 1.9209 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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