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Purity: ≥98%
Lofexidine HCl (Lucemyra) is the hydrochloride salt of lofexidine which is an analog of Clonidine and an α2A adrenergic receptor agonist. This drug is authorized for the treatment of hypertension; however, it is primarily utilized to ease the physical manifestations of opioid withdrawal symptoms.
| Molecular Formula |
C11H13CL3N2O
|
|---|---|
| Molecular Weight |
295.59
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| Exact Mass |
294.01
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| Elemental Analysis |
C, 44.70; H, 4.43; Cl, 35.98; N, 9.48; O, 5.41
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| CAS # |
21498-08-8
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| Related CAS # |
Lofexidine; 31036-80-3; Lofexidine-d4 hydrochloride; 1206845-57-9
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| Appearance |
Solid powder
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| SMILES |
CC(C1=NCCN1)OC2=C(C=CC=C2Cl)Cl.Cl
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| InChi Key |
DWWHMKBNNNZGHF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H12Cl2N2O.ClH/c1-7(11-14-5-6-15-11)16-10-8(12)3-2-4-9(10)13;/h2-4,7H,5-6H2,1H3,(H,14,15);1H
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| Chemical Name |
2-[1-(2,6-dichlorophenoxy)ethyl]-4,5-dihydro-1H-imidazole;hydrochloride
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| Synonyms |
Lofexidine Hydrochloride; Lofetensin; Brand name Lucemyra; Lofexidine HCl; Loxacor;Lofexidine mono-hydrochloride; lofexidine (+-)-isomer
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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, 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.04 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 20.8 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: ≥ 2.08 mg/mL (7.04 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 20.8 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: ≥ 2.08 mg/mL (7.04 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (338.31 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3831 mL | 16.9153 mL | 33.8306 mL | |
| 5 mM | 0.6766 mL | 3.3831 mL | 6.7661 mL | |
| 10 mM | 0.3383 mL | 1.6915 mL | 3.3831 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03718065 | Recruiting | Drug: Lofexidine Drug: Placebo |
Opioid-use Disorder Opiate Dependence |
Medical University of South Carolina |
June 26, 2019 | Phase 2 |
| NCT05712707 | Recruiting | Other: Placebo Drug: albuterol Sulfate |
Asthma COPD |
Sumitomo Pharma America, Inc. | March 2003 | Phase 4 |
| NCT00667407 | Recruiting | Drug: Levalbuterol 1.25 mg Other: Lofexidine (Positive Control) |
Opioid Use Disorder Opioid Withdrawal |
New York State Psychiatric Institute |
February 28, 2023 | Phase 1 Phase 2 |
| NCT04325659 | Recruiting | Drug: Lofexidine Drug: Placebo |
Opioid Dependence Opioid Addiction |
Johns Hopkins University | November 15, 2020 | Phase 2 Phase 3 |
| NCT05511909 | Recruiting | Drug: Lofexidine Drug: Placebo |
Opioid Use Disorder Anxiety |
Johns Hopkins University | December 15, 2022 | Phase 2 |
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