| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| Other Sizes |
| Targets |
Etilevodopa HCl targets the dopaminergic system in the brain. As a prodrug of levodopa, it is converted to levodopa, which is then decarboxylated to dopamine by aromatic L-amino acid decarboxylase (AADC) in the brain. Dopamine acts on dopamine receptors to restore dopaminergic neurotransmission in Parkinson's disease. The compound also targets peripheral AADC, but this is typically inhibited by co-administered carbidopa.
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| ln Vitro |
After traveling through the stomach unaltered, ativodopa (levodopa ethyl ester) hydrochloride enters the duodenum, where local esterase quickly hydrolyzes it into levodopa and ethanol, which is then quickly absorbed into the bloodstream as levodopa. Stream [1]. Azidovopa hydrochloride is more soluble in the stomach, enters the small intestine more quickly, and achieves the maximum levodopa concentration in less time when compared to regular levodopa [2].
In vitro, Etilevodopa HCl is converted to levodopa by esterase-mediated hydrolysis. Levodopa is then decarboxylated to dopamine by AADC. The compound's stability and conversion kinetics are studied in vitro using liver or plasma esterases. Specific kinetic parameters for hydrolysis are available from biochemical assays. |
| ln Vivo |
In vivo, Etilevodopa HCl is a prodrug of levodopa used for the treatment of Parkinson's disease. It improves the oral bioavailability of levodopa compared to levodopa alone. After absorption, Etilevodopa is hydrolyzed to levodopa, which crosses the blood-brain barrier and is converted to dopamine. The compound is typically administered in combination with carbidopa to inhibit peripheral decarboxylation.
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| Enzyme Assay |
The in vitro hydrolysis assay for Etilevodopa HCl involves measuring its conversion to levodopa by esterases. Liver or plasma esterases are incubated with varying concentrations of Etilevodopa HCl, and the formation of levodopa is measured by HPLC or mass spectrometry. The kinetic parameters (Km, Vmax) for hydrolysis are determined. The compound's stability in various biological matrices is also assessed.
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| Cell Assay |
In vitro cellular assays for Etilevodopa HCl involve treating cultured cells expressing AADC with varying concentrations of the compound or its metabolite levodopa. Dopamine production is measured by HPLC or ELISA. The compound's ability to increase dopamine levels in cells is assessed. Cell viability and toxicity are evaluated using MTT assays.
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| Animal Protocol |
In vivo animal experiments for Etilevodopa HCl typically use rodent or primate models of Parkinson's disease. The compound is administered orally at various doses, with or without carbidopa. Brain dopamine levels are measured by microdialysis or tissue homogenate analysis. Behavioral tests, including locomotor activity and motor coordination, are performed to assess efficacy.
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| ADME/Pharmacokinetics |
Etilevodopa HCl has a molecular weight of 245.66 (C11H15NO4·HCl). As a prodrug of levodopa, it is administered orally and is hydrolyzed to levodopa by esterases. The compound has improved oral bioavailability compared to levodopa. Specific PK parameters including half-life, Cmax, and AUC are available from clinical pharmacology studies.
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| Toxicity/Toxicokinetics |
Etilevodopa HCl is used in the treatment of Parkinson's disease as a prodrug of levodopa. Common adverse effects are similar to those of levodopa and may include nausea, vomiting, dyskinesia, and orthostatic hypotension. The compound is typically co-administered with carbidopa to reduce peripheral side effects. Complete toxicology data are available from the drug's clinical development program.
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| References |
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| Additional Infomation |
Etilevodopa HCl (CAS#: 39740-30-2) is the hydrochloride salt of the ethyl ester prodrug of levodopa, designed to improve the oral bioavailability of levodopa for the treatment of Parkinson's disease. It is converted to levodopa in the body, which then crosses the blood-brain barrier and is converted to dopamine. Etilevodopa HCl is typically administered in combination with carbidopa. The compound is used clinically in some regions.
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| Molecular Formula |
C11H16CLNO4
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|---|---|
| Molecular Weight |
261.702
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| Exact Mass |
261.077
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| Elemental Analysis |
C, 50.49; H, 6.16; Cl, 13.55; N, 5.35; O, 24.45
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| CAS # |
39740-30-2
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| Related CAS # |
Etilevodopa;37178-37-3
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| PubChem CID |
12485237
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.033
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
17
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| Complexity |
234
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CCOC(=O)[C@H](CC1=CC(=C(C=C1)O)O)N.Cl
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| InChi Key |
CVQFXVIIFKVRCK-QRPNPIFTSA-N
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| InChi Code |
InChI=1S/C11H15NO4.ClH/c1-2-16-11(15)8(12)5-7-3-4-9(13)10(14)6-7;/h3-4,6,8,13-14H,2,5,12H2,1H3;1H/t8-;/m0./s1
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| Chemical Name |
ethyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate;hydrochloride
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| Synonyms |
TV-1203 HCl; L-Dopa ethyl ester; L-DOPA Ethyl Ester Hydrochloride; Levodopa ethyl ester; TV1203; Etilevodopa
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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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), 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 : ~125 mg/mL (~477.65 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 25 mg/mL (95.53 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8212 mL | 19.1058 mL | 38.2117 mL | |
| 5 mM | 0.7642 mL | 3.8212 mL | 7.6423 mL | |
| 10 mM | 0.3821 mL | 1.9106 mL | 3.8212 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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