| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
The active metabolite α-methylnorepinephrine acts as an α2-adrenergic receptor agonist in the brainstem, reducing sympathetic tone and lowering blood pressure; the prodrug methyldopate itself is hydrolyzed to methyldopa, which is a dopamine decarboxylase inhibitor and is further metabolized to the active α2 agonist.
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|---|---|
| ln Vitro |
Methyldopate is used in vitro as a prodrug form of methyldopa in enzymatic assays of dopamine decarboxylase inhibition and in cell-based systems to study catecholamine metabolism; it lacks intrinsic receptor-binding activity until hydrolyzed and metabolized, and its in vitro antihypertensive activity is therefore assessed after conversion to active metabolites in tissue preparations.
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| ln Vivo |
Methyldopa is degraded to methyldopa in the body [2].
In vivo, methyldopate is rapidly degraded to methyldopa and produces antihypertensive effects in animal models of hypertension; it lowers blood pressure through central α2-adrenergic agonism, reduces peripheral sympathetic tone, and is used in research to study hypertension mechanisms in both acute and chronic dosing paradigms. |
| Enzyme Assay |
Dopamine decarboxylase activity is measured in tissue homogenates or partially purified enzyme preparations incubated with L-DOPA or a fluorescent substrate in the presence of graded methyldopate or methyldopa concentrations; product formation is quantified by HPLC or fluorescence, and IC50 values are calculated; receptor-binding assays for α2-adrenergic receptors use brainstem membranes and a suitable radioligand.
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| Cell Assay |
Cell or tissue preparations (e.g., brainstem synaptosomes or catecholaminergic cell lines) are incubated with methyldopate or its active metabolites, and dopamine decarboxylase activity, catecholamine content, or α2-adrenergic receptor signaling (e.g., cAMP inhibition, GTPγS binding) is measured; viability and metabolic activity assays are used to assess nonspecific toxicity.
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| Animal Protocol |
Hypertensive rats or dogs receive methyldopate by oral or intravenous administration at doses selected from pharmacokinetic and tolerability studies; blood pressure and heart rate are monitored by tail-cuff or telemetry, plasma and tissue catecholamine metabolites are quantified by HPLC, and central α2-adrenergic receptor occupancy is inferred from functional responses to α2 agonists and antagonists.
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| References |
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| Additional Infomation |
Alpha-methyl-L-dopa ethyl ester is an ethyl ester derivative of alpha-methyl-L-dopa. It is an alpha-adrenergic agonist and antihypertensive drug. It belongs to the amphetamine class of drugs and is an ethyl ester compound. Its function is related to alpha-methyl-L-dopa. Alpha-methyl-L-dopa is an alpha-2 adrenergic agonist with effects on both the central and peripheral nervous systems. Its primary clinical use is as an antihypertensive drug.
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| Molecular Formula |
C12H17NO4
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|---|---|
| Molecular Weight |
239.2677
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| Exact Mass |
239.115
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| CAS # |
6014-30-8
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| Related CAS # |
Methyldopate hydrochloride;2508-79-4
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| PubChem CID |
17277
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| Appearance |
Light brown to brown solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
398.0±37.0 °C at 760 mmHg
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| Flash Point |
194.5±26.5 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.573
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| LogP |
0.81
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| Hydrogen Bond Donor Count |
3
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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 |
271
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CCOC(=O)[C@](C)(CC1=CC(=C(C=C1)O)O)N
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| InChi Key |
SVEBYYWCXTVYCR-LBPRGKRZSA-N
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| InChi Code |
InChI=1S/C12H17NO4/c1-3-17-11(16)12(2,13)7-8-4-5-9(14)10(15)6-8/h4-6,14-15H,3,7,13H2,1-2H3/t12-/m0/s1
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| Chemical Name |
ethyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)-2-methylpropanoate
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~100 mg/mL (~417.94 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.45 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 25.0 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: ≥ 2.5 mg/mL (10.45 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 25.0 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: ≥ 2.5 mg/mL (10.45 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 | 4.1794 mL | 20.8969 mL | 41.7938 mL | |
| 5 mM | 0.8359 mL | 4.1794 mL | 8.3588 mL | |
| 10 mM | 0.4179 mL | 2.0897 mL | 4.1794 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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