Levonordefrin
Based on 1 Customer Validation
Levonordefrin ((-)-Cobefrin; (-)-α-Methylnoradrenaline; (-)-Nordefrin) is an α-adrenergic receptor agonist with blood pressure regulatory properties. Levonordefrin is a key metabolite responsible for the hypotensive effect of α-methyldopa. By stimulating central α-adrenergic receptors in the nucleus tractus solitarius region of the medulla oblongata, Levonordefrin induces centrally mediated hypotension and bradycardia. When administered intravenously, Levonordefrin increases mean arterial blood pressure in a dose-dependent manner. Levonordefrin is applicable for research on the pathophysiology of hypertension and drug metabolism.
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- Pureza: 98.38%
- No. CAS: 829-74-3
- Fòrmula: C9H13NO3
- Peso molecular:183.21
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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α1-adrenergic receptor |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats (male, 200-250 g, anesthetized with urethane)[2]
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Dosage:5.8 nmol; 23.0 nmol; 92.0 nmol; 23.0 nmol (post-Phentolamine pre-treatment)
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Administration:bilateral microinjection into nucleus tractus solitarii; 0.6 μL over 30 seconds; 23.0 nmol (10 minutes after phentolamine microinjection)
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Result:Caused a maximum mean blood pressure decrease of -16 ± 2 mm Hg and heart rate decrease of -27 ± 11 bpm at 5 minutes, with effects resolved by 30 minutes (blood pressure +1 ± 26 mm Hg, heart rate +42 ± 26 bpm) at 5.8 nmol.
Caused sustained, statistically significant (p < 0.01) decreases in mean blood pressure and heart rate through 30 minutes: -33 ± 6 mm Hg/-56 ± 14 bpm at 5 minutes, -33 ± 6 mm Hg/-66 ± 7 bpm at 10 minutes, -23 ± 5 mm Hg/-43 ± 7 bpm at 20 minutes, -15 ± 4 mm Hg/-28 ± 9 bpm at 30 minutes at 23.0 nmol.
Caused sustained, statistically significant (p < 0.01) decreases in mean blood pressure and heart rate through 30 minutes: -39 ± 5 mm Hg/-38 ± 7 bpm at 5 minutes, -43 ± 4 mm Hg/-75 ± 11 bpm at 10 minutes, -32 ± 3 mm Hg/-86 ± 11 bpm at 20 minutes, -20 ± 3 mm Hg/-74 ± 14 bpm at 30 minutes at 92.0 nmol.
Produced maximum changes of +31 ± 6 mm Hg (blood pressure) and +27 ± 9 bpm (heart rate) within 2 minutes when 23.0 nmol was administered 10 minutes after prior phentolamine microinjection, completely preventing and reversing hypotensive and bradycardic effects.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 829-74-3
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Appearance Solid
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Peso molecular 183.21
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Fòrmula C9H13NO3
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Color Off-white to light brown
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SMILES
OC1=CC=C([C@@H](O)[C@@H](N)C)C=C1O
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Synonyms
(-)-Cobefrin; (-)-α-Methylnoradrenaline; (-)-Nordefrin
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 50 mg/mL (272.91 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 5 mg/mL (27.29 mM; ultrasonic and warming and adjust pH to 1 with HCl and heat to 60°C)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (13.65 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (13.65 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (394 KB)
- English - EN (394 KB)
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- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 5.4582 mL | 27.2911 mL | 54.5822 mL | 136.4554 mL |
| 5 mM | 1.0916 mL | 5.4582 mL | 10.9164 mL | 27.2911 mL | |
| 10 mM | 0.5458 mL | 2.7291 mL | 5.4582 mL | 13.6455 mL | |
| 15 mM | 0.3639 mL | 1.8194 mL | 3.6388 mL | 9.0970 mL | |
| 20 mM | 0.2729 mL | 1.3646 mL | 2.7291 mL | 6.8228 mL | |
| 25 mM | 0.2183 mL | 1.0916 mL | 2.1833 mL | 5.4582 mL | |
| DMSO | 30 mM | 0.1819 mL | 0.9097 mL | 1.8194 mL | 4.5485 mL |
| 40 mM | 0.1365 mL | 0.6823 mL | 1.3646 mL | 3.4114 mL | |
| 50 mM | 0.1092 mL | 0.5458 mL | 1.0916 mL | 2.7291 mL | |
| 60 mM | 0.0910 mL | 0.4549 mL | 0.9097 mL | 2.2743 mL | |
| 80 mM | 0.0682 mL | 0.3411 mL | 0.6823 mL | 1.7057 mL | |
| 100 mM | 0.0546 mL | 0.2729 mL | 0.5458 mL | 1.3646 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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