MedKoo Cat#: 599157 | Name: Lofexidine
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Lofexidine reduces narcotic withdrawal symptoms.

Chemical Structure

Lofexidine
Lofexidine
CAS#31036-80-3 (free base)

Theoretical Analysis

MedKoo Cat#: 599157

Name: Lofexidine

CAS#: 31036-80-3 (free base)

Chemical Formula: C11H12Cl2N2O

Exact Mass: 258.0327

Molecular Weight: 259.13

Elemental Analysis: C, 50.99; H, 4.67; Cl, 27.36; N, 10.81; O, 6.17

Price and Availability

Size Price Availability Quantity
100mg USD 450.00 2 weeks
250mg USD 850.00 2 weeks
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Synonym
Lofexidine; Loxacor; MDL 14,042; MDL-14,042; MDL14,042; RMI-14042A; RMI14042A; RMI 14042A; BA 168; Lofetensin; Lucemyra
IUPAC/Chemical Name
2-(1-(2,6-dichlorophenoxy)ethyl)-4,5-dihydro-1H-imidazole
InChi Key
KSMAGQUYOIHWFS-UHFFFAOYSA-N
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)
SMILES Code
CC(C1=NCCN1)OC2=C(Cl)C=CC=C2Cl
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Biological target:
Lofexidine is a selective α2-receptor agonist.
In vitro activity:
TBD
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMSO 62.5 241.19
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 259.13 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
TBD
In vitro protocol:
TBD
In vivo protocol:
TBD
1: Kuszmaul AK, Palmer EC, Frederick EK. Lofexidine versus clonidine for mitigation of opioid withdrawal symptoms: A systematic review. J Am Pharm Assoc (2003). 2019 Nov 29. pii: S1544-3191(19)30453-4. doi: 10.1016/j.japh.2019.10.004. [Epub ahead of print] Review. PubMed PMID: 31791720. 2: Rehman SU, Maqsood MH, Bajwa H, Tameez Ud Din A, Malik MN. Clinical Efficacy and Safety Profile of Lofexidine Hydrochloride in Treating Opioid Withdrawal Symptoms: A Review of Literature. Cureus. 2019 Jun 4;11(6):e4827. doi: 10.7759/cureus.4827. Review. PubMed PMID: 31403015; PubMed Central PMCID: PMC6682385. 3: Pergolizzi JV Jr, Annabi H, Gharibo C, LeQuang JA. The Role of Lofexidine in Management of Opioid Withdrawal. Pain Ther. 2019 Jun;8(1):67-78. doi: 10.1007/s40122-018-0108-7. Epub 2018 Dec 18. Review. PubMed PMID: 30565033; PubMed Central PMCID: PMC6513979. 4: Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006-. Available from http://www.ncbi.nlm.nih.gov/books/NBK513054/ PubMed PMID: 30000984. 5: Gish EC, Miller JL, Honey BL, Johnson PN. Lofexidine, an {alpha}2-receptor agonist for opioid detoxification. Ann Pharmacother. 2010 Feb;44(2):343-51. doi: 10.1345/aph.1M347. Epub 2009 Dec 29. Review. PubMed PMID: 20040696. 6: Strang J, Bearn J, Gossop M. Lofexidine for opiate detoxification: review of recent randomised and open controlled trials. Am J Addict. 1999 Fall;8(4):337-48. Review. PubMed PMID: 10598217. 7: Cox S, Alcorn R. Lofexidine and opioid withdrawal. Lancet. 1995 Jun 3;345(8962):1385-6. Review. PubMed PMID: 7760607.