Lofexidine
Based on 1 Customer Validation
Lofexidine (Baq-168 free base) is an orally active agonist of the imidazoline I1 receptor (imidazoline I1 receptor) (Ki: 1.9 nM) and α2-adrenergic receptor (α2-adrenergic receptor). Lofexidine binds to the α2A-adrenergic receptor, reduces sympathetic outflow, lowers blood pressure, and exhibits vasoconstrictive effects. Lofexidine regulates the expression of c-fos and alleviates opioid withdrawal symptoms. Lofexidine is applicable to research on opioid addiction and withdrawal.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.08%
- No. CAS: 31036-80-3
- Fòrmula: C11H12Cl2N2O
- Peso molecular:259.13
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Actividad biológica
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α adrenergic receptor |
Lofexidine binds to α2-adrenergic receptors in rat brain cell membranes, with a Kd value of 5.5 nM[1].
Lofexidine induces peripheral vasoconstriction in isolated rabbit ear central artery specimens[1].
Lofexidine attenuates norepinephrine-induced contraction responses of isolated vas deferens specimens in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Lofexidine (Intravenous administration) induces a transient hypertensive response followed by sustained hypotension in dogs and cats, whereas oral administration only causes hypotension[1].
Lofexidine reduces the expression of Fos protein in the locus coeruleus of morphine-addicted mice during opioid withdrawal[1].
Lofexidine (p.o.) induces reversible neurological symptoms in rats and dogs, with an LD50 of 70-147 mg/kg in rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats and dogs[2]
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Dosage:/
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Administration:p.o.; daily; 1 week (chronic)
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Result:Caused sedation, ataxia, exophthalmia, hyperexcitability, and convulsions that resolved by day 2.
Found LD50 between 70 and 147 mg/kg in rats.
Caused liver function test elevations that did not exceed the upper normal limit.
Chemical Information
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No. CAS 31036-80-3
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Appearance Solid
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Peso molecular 259.13
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Fòrmula C11H12Cl2N2O
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Color White to off-white
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SMILES
CC(C1=NCCN1)OC2=C(Cl)C=CC=C2Cl
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Synonyms
Baq-168 free base; MDL-14042 free base
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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 : 62.5 mg/mL (241.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
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: ≥ 2.08 mg/mL (8.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (8.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.8591 mL | 19.2953 mL | 38.5907 mL | 96.4767 mL |
| 5 mM | 0.7718 mL | 3.8591 mL | 7.7181 mL | 19.2953 mL | |
| 10 mM | 0.3859 mL | 1.9295 mL | 3.8591 mL | 9.6477 mL | |
| 15 mM | 0.2573 mL | 1.2864 mL | 2.5727 mL | 6.4318 mL | |
| 20 mM | 0.1930 mL | 0.9648 mL | 1.9295 mL | 4.8238 mL | |
| 25 mM | 0.1544 mL | 0.7718 mL | 1.5436 mL | 3.8591 mL | |
| 30 mM | 0.1286 mL | 0.6432 mL | 1.2864 mL | 3.2159 mL | |
| 40 mM | 0.0965 mL | 0.4824 mL | 0.9648 mL | 2.4119 mL | |
| 50 mM | 0.0772 mL | 0.3859 mL | 0.7718 mL | 1.9295 mL | |
| 60 mM | 0.0643 mL | 0.3216 mL | 0.6432 mL | 1.6079 mL | |
| 80 mM | 0.0482 mL | 0.2412 mL | 0.4824 mL | 1.2060 mL | |
| 100 mM | 0.0386 mL | 0.1930 mL | 0.3859 mL | 0.9648 mL |
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