| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 500mg |
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| Targets |
Etilefrine targets α1 and β1 adrenergic receptors. It acts as an adrenergic agonist, selectively binding to and activating α1-adrenergic receptors in arterioles and veins. Activation of α1 receptors causes smooth muscle contraction, leading to vasoconstriction and increased peripheral resistance. β1 receptor activation enhances myocardial contractility and elevates heart rate.
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| ln Vitro |
In vitro, Etilefrine acts as an adrenergic agonist, stimulating α1 and β1 adrenergic receptors. It activates AMPK and induces vasoconstriction in isolated vascular preparations. The compound's activity at α1 receptors leads to contraction of vascular smooth muscle. Specific IC50 or EC50 values for receptor activation are not extensively documented in publicly available literature.
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| ln Vivo |
Blood pressure (BP) and heart rate (HR) are raised by etifulin (0.1 mg/kg; IV); however, the tilt-induced drop in BP is not mitigated by etifulin. Furthermore, etifoline raises cardiac output (CO) [3].
In vivo, Etilefrine is used as a vasoconstrictor for the treatment of orthostatic hypotension. It increases blood pressure by stimulating α1 receptors, leading to vasoconstriction and decreased venous pooling. β1 receptor activation enhances cardiac contractility and output. The compound has been studied for the treatment of levodopa-induced orthostatic hypotension. |
| Enzyme Assay |
The in vitro receptor binding assay for Etilefrine involves measuring its affinity for α1 and β1 adrenergic receptors. Radiolabeled ligand binding assays are performed using membrane preparations from cells expressing α1 or β1 receptors. Varying concentrations of Etilefrine are incubated with the receptor preparation, and binding affinity (IC50 or Ki) is determined. Etilefrine acts as an agonist at α1 and β1 receptors, stimulating downstream signaling pathways.
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| Cell Assay |
In vitro cellular assays for Etilefrine involve treating cultured vascular smooth muscle cells or cardiomyocytes with varying concentrations of the compound. Receptor activation is assessed by measuring intracellular calcium mobilization or cAMP levels. Smooth muscle contraction is measured using isolated vessel preparations. AMPK activation is assessed by Western blotting for phosphorylated AMPK.
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| Animal Protocol |
In vivo animal experiments for Etilefrine typically use rodent models of orthostatic hypotension or shock. The compound is administered via intravenous or oral routes at various doses. Blood pressure and heart rate are measured using tail-cuff or telemetry methods. Vasoconstriction is assessed by measuring peripheral resistance. The compound's pressor effects are compared to reference vasoconstrictors.
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| ADME/Pharmacokinetics |
Etilefrine has a half-life of approximately 2-2.5 hours. It is subject to significant first-pass metabolism, leading to a bioavailability of about 30-40%. The compound has a molecular weight of 181.23 (C10H15NO2). Etilefrine is metabolized in the liver and excreted via the kidneys. A washout period of at least 12.5 hours is recommended for pharmacokinetic studies.
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| Toxicity/Toxicokinetics |
Etilefrine is a clinically used vasoconstrictor with an established safety profile. Common adverse effects may include hypertension, tachycardia, palpitations, and headache. The compound is contraindicated in patients with severe hypertension, pheochromocytoma, or tachyarrhythmias. Regular monitoring of blood pressure and heart rate is required during treatment. Complete toxicology data are available from the drug's clinical use.
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| References |
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| Additional Infomation |
3-[2-(ethylamino)-1-hydroxyethyl]phenol belongs to the phenolic class of compounds. Etilefrinee is an adrenergic agonist that appears to interact with β1 and certain α-adrenergic receptors. It has been used as a vasoconstrictor. Etilefrinee is an adrenergic agonist with vasoconstrictive activity. Etilefrinee selectively binds to and activates α1-adrenergic receptors in arterioles and veins. This leads to smooth muscle contraction, thereby reducing venous blood pooling and increasing blood pressure. The drug may also stimulate β1-adrenergic receptors, producing positive chronotropic and positive inotropic effects. A phenyladrenergic β1-adrenergic and α-adrenergic agonist used as a cardiotonic and antihypertensive agent. See also: Etilefrine hydrochloride (note moved to).
Etilefrine (CAS#: 709-55-7) is a sympathetic nerve agonist and AMPK activator that selectively targets α1 and β1 adrenergic receptors. It is used as a vasoconstrictor for the treatment of orthostatic hypotension. Etilefrine stimulates α1 receptors to cause vasoconstriction and increased peripheral resistance, and activates β1 receptors to enhance cardiac contractility. The compound has a half-life of approximately 2-2.5 hours and is subject to first-pass metabolism. |
| Molecular Formula |
C10H15NO2
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|---|---|
| Molecular Weight |
181.2316
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| Exact Mass |
181.11
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| CAS # |
709-55-7
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| Related CAS # |
Etilefrine hydrochloride;943-17-9
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| PubChem CID |
3306
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| Appearance |
Off-white to pink solid powder
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| Density |
1.127 g/cm3
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| Boiling Point |
351.7ºC at 760 mmHg
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| Melting Point |
208-209
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| Flash Point |
155.5ºC
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| Index of Refraction |
1.561
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| LogP |
1.426
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
13
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| Complexity |
141
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SQVIAVUSQAWMKL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H15NO2/c1-2-11-7-10(13)8-4-3-5-9(12)6-8/h3-6,10-13H,2,7H2,1H3
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| Chemical Name |
3-[2-(ethylamino)-1-hydroxyethyl]phenol
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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 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
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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 | 5.5179 mL | 27.5893 mL | 55.1785 mL | |
| 5 mM | 1.1036 mL | 5.5179 mL | 11.0357 mL | |
| 10 mM | 0.5518 mL | 2.7589 mL | 5.5179 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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