| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
HepG2 human hepatoma cells can produce and release [35S] sulfated metabolites of catechol medicines when exposed to isoethylamine at a concentration of 50 μM for eighteen hours [1].
|
|---|---|
| ln Vivo |
In the zebrafish larval model, isoethyl can suppress melanin deposition with an AC50 value of 5.10 mM, while 7.50 mM can fully block pigment formation [2].
|
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Isoetharine is rapidly metabolized once inhaled. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Isoetharine is no longer marketed in the US. Although no published data exist on the use of isoetharine during lactation, data from the related drug, terbutaline, indicate that very little is expected to be excreted into breastmilk. The authors of several reviews and an expert panel agree that use of inhaled bronchodilators is acceptable during breastfeeding because of the low bioavailability and maternal serum levels after use. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
| References |
[1]. Katsuhisa Kurogi，et al. Concerted actions of the catechol O-methyltransferase and the cytosolic sulfotransferase SULT1A3 in the metabolism of catecholic drugs. Biochem Pharmacol. 2012 Nov 1;84(9):1186-95.
[2]. Monika Maciag，et al. Evaluation of β-adrenergic ligands for development of pharmacological heart failure and transparency models in zebrafish. Toxicol Appl Pharmacol. 2022 Jan 1;434:115812. |
| Additional Infomation |
Isoetharine is a catecholamine.
Isoetharine is a relatively selective beta-2 adrenergic agonist. It is a catechol-like agent. Isoetharine is a fast-acting bronchodilator used for emphysema, bronchitis and asthma. Isoetharine is a beta-adrenergic receptor agonist with bronchodilator activity. Isoetharine selectively binds to beta-2 adrenergic receptors in bronchial smooth muscle, thereby activating intracellular adenyl cyclase, an enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP). Increased cAMP levels cause relaxation of bronchial smooth muscle, relieve bronchospasms, improve mucociliary clearance and reduce mediator substance release from inflammatory cells, especially from mast cells. Adrenergic beta-2 agonist used as bronchodilator for emphysema, bronchitis and asthma. Drug Indication For the treatment of asthma, wheezing, and chronic asthmatic bronchitis. Mechanism of Action Isoetharine-induced bronchodilator occurs from an increased activity of adenyl cyclase, which augments the formation of cyclic AMP (cAMP). Increased levels of cAMP result in the relaxation of bronchial smooth muscle, stimulation of ciliary activity, and potential improvement in capillary integrity. Pharmacodynamics Isoetharine is a beta-adrenergic receptor agonist. While it is reported to demonstrate more selectivity towards beta-2 adrenergic receptors, isoetharine still binds to beta-1 adrenergic receptors and thus may be associated with beta-1-mediated adverse events. Isoetharine produces maximal bronchodilation within 15 minutes of inhalation. |
| Molecular Formula |
C13H21NO3
|
|---|---|
| Molecular Weight |
239.31074
|
| Exact Mass |
239.152
|
| CAS # |
530-08-5
|
| Related CAS # |
Isoetharine mesylate;7279-75-6;Isoetharine hydrochloride;50-96-4
|
| PubChem CID |
3762
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
2.298
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
17
|
| Complexity |
223
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CCC(C(C1=CC(=C(C=C1)O)O)O)NC(C)C
|
| InChi Key |
HUYWAWARQUIQLE-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C13H21NO3/c1-4-10(14-8(2)3)13(17)9-5-6-11(15)12(16)7-9/h5-8,10,13-17H,4H2,1-3H3
|
| Chemical Name |
4-[1-hydroxy-2-(propan-2-ylamino)butyl]benzene-1,2-diol
|
| 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 (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
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 | 4.1787 mL | 20.8934 mL | 41.7868 mL | |
| 5 mM | 0.8357 mL | 4.1787 mL | 8.3574 mL | |
| 10 mM | 0.4179 mL | 2.0893 mL | 4.1787 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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