| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
Alpha-1 adrenergic receptor; dopamine β-oxidase; norepinephrine transporter (NET). Adrenalone is an alpha-1 adrenergic receptor agonist, causing vasoconstriction and hemostasis when applied topically. It is also an inhibitor of dopamine β-oxidase and binds to the norepinephrine transporter with an IC50 of 36.9 μM.
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| ln Vitro |
adrenaline, the ketone form of the natural substrate adrenaline, is a local nasal decongestant, hemostatic, and vasoconstrictor [1]. Dopamine beta-oxidase activity is inhibited by epinephrine. Substrate transport in NETs is inhibited by epinephrine [2].
Adrenalone acts as an alpha-1 adrenergic receptor agonist in vitro, causing vasoconstriction. It inhibits dopamine β-oxidase activity and binds to the norepinephrine transporter with an IC50 of 36.9 μM. The compound's potency and efficacy have been characterized in various receptor binding and functional assays. |
| ln Vivo |
In vivo, Adrenalone is used as a topical vasoconstrictor and hemostatic agent. It is applied locally to reduce bleeding and vascular congestion. The compound's vasoconstrictive effects are mediated through alpha-1 adrenergic receptor activation. It is chemically similar to epinephrine but has different pharmacokinetic properties.
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| Enzyme Assay |
In vitro receptor binding assays for Adrenalone involve competition binding experiments using radiolabeled ligands such as [3H]-prazosin for alpha-1 adrenergic receptors. Membranes are prepared from cells expressing the alpha-1 receptor. Adrenalone is incubated at varying concentrations, and bound radioactivity is measured. Ki values are calculated from displacement curves. NET binding assays can also be performed.
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| Cell Assay |
Cellular assays for Adrenalone involve culturing cells expressing alpha-1 adrenergic receptors. Cells are treated with Adrenalone at varying concentrations (typically 0.1-100 µM). Calcium mobilization is measured using fluorescent indicators. The compound's agonist activity is assessed by its ability to increase intracellular calcium levels. Dopamine β-oxidase inhibition assays can be performed using cell lysates or purified enzyme.
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| Animal Protocol |
In vivo animal studies for Adrenalone are typically conducted in rodent models to assess its vasoconstrictive and hemostatic effects. The compound is applied topically, and bleeding time or vascular diameter is measured. Dosing regimens vary depending on the study objectives. The compound is not typically administered systemically.
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| ADME/Pharmacokinetics |
Adrenalone has a molecular weight of 181.19 g/mol and a molecular formula of C9H11NO3. Its chemical name is 1-(3,4-dihydroxyphenyl)-2-(methylamino)ethanone hydrochloride. The compound is soluble in water and should be stored at room temperature protected from light. It is available with a purity of ≥98%. Detailed pharmacokinetic parameters are not extensively documented.
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| Toxicity/Toxicokinetics |
Adrenalone is generally well-tolerated when used as a topical agent. Systemic absorption is minimal. The compound may cause local irritation or allergic reactions. It is contraindicated in patients with hypersensitivity to adrenergic agents. The compound is not approved for systemic use. Standard safety precautions should be taken when handling the compound.
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| References |
[1]. M GOLDSTEIN,et al. Inhibition of dopamine beta oxidase by adrenalone. Nature.1961 Dec 16;192:1081.
[2]. Avner Schlessinger, et al. Structure-based discovery of prescription drugs that interact with the norepinephrine transporter, NET. Proc Natl Acad Sci U S A. 2011 Sep 20;108(38):15810-5. |
| Additional Infomation |
Adrenosterone is an aromatic ketone.
Adrenalone is a synthetic catecholamine derivative and alpha-1 adrenergic receptor agonist used as a topical vasoconstrictor and hemostatic agent. It is also an inhibitor of dopamine β-oxidase and binds to the norepinephrine transporter. The compound is not approved for systemic use and is available for research and topical applications. |
| Molecular Formula |
C9H11NO3
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|---|---|
| Molecular Weight |
181.18854
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| Exact Mass |
181.073
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| CAS # |
99-45-6
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| Related CAS # |
Adrenalone hydrochloride;62-13-5
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| PubChem CID |
7436
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
405.6±40.0 °C at 760 mmHg
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| Melting Point |
235.5°C (rough estimate)
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| Flash Point |
199.1±27.3 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.589
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| LogP |
0.67
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
13
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| Complexity |
184
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CNCC(=O)C1=CC(=C(C=C1)O)O
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| InChi Key |
PZMVOUYYNKPMSI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H11NO3/c1-10-5-9(13)6-2-3-7(11)8(12)4-6/h2-4,10-12H,5H2,1H3
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| Chemical Name |
1-(3,4-dihydroxyphenyl)-2-(methylamino)ethanone
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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 | 5.5191 mL | 27.5953 mL | 55.1907 mL | |
| 5 mM | 1.1038 mL | 5.5191 mL | 11.0381 mL | |
| 10 mM | 0.5519 mL | 2.7595 mL | 5.5191 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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