Size | Price | Stock | Qty |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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2g |
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Other Sizes |
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Purity: ≥98%
Lofexidine (Lofetensin; Loxacor; brand name Lucemyra among others), an analog of Clonidine, is a medication historically used to treat high blood pressure, but nowadays, it is more commonly used to help with the physical symptoms of opioid withdrawal. Lofexidine is an agonist of the α2A adrenergic receptor that the Food and Drug Administration of the United States approved for use in 2018. Although it has been studied, the efficacy of lofexidine as a treatment for alcohol withdrawal symptoms has not yet been demonstrated. Additionally, postmenopausal hot flash sufferers are treated with it.
Molecular Formula |
C11H12CL2N2O
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Molecular Weight |
259.13
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Exact Mass |
258.03
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Elemental Analysis |
C, 50.99; H, 4.67; Cl, 27.36; N, 10.81; O, 6.17
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CAS # |
31036-80-3
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Related CAS # |
Lofexidine hydrochloride; 21498-08-8
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Appearance |
Solid powder
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SMILES |
CC(C1=NCCN1)OC2=C(C=CC=C2Cl)Cl
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InChi Key |
KSMAGQUYOIHWFS-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C11H12Cl2N2O/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)
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Chemical Name |
2-[1-(2,6-dichlorophenoxy)ethyl]-4,5-dihydro-1H-imidazole
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Synonyms |
RMI-14042A; MDL-14,042; MDL 14,042; MDL14,042; Lofexidine; Loxacor; RMI14042A; RMI 14042A; BA 168; Lofetensin; Lucemyra
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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 |
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 (8.03 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 (8.03 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 (8.03 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 | 3.8591 mL | 19.2953 mL | 38.5907 mL | |
5 mM | 0.7718 mL | 3.8591 mL | 7.7181 mL | |
10 mM | 0.3859 mL | 1.9295 mL | 3.8591 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 |