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MedKoo Cat#: 318158 | Name: Lofexidine Hydrochloride
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Description:

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

Lofexidine Hydrochloride is an alpha2-adrenergic receptor agonist that is structurally related to Clonidine and used in the treatment of opioid withdrawal symptoms as well as an anihypertensive. It can be used as a short acting anti-hypertensive.

Chemical Structure

Lofexidine Hydrochloride
Lofexidine Hydrochloride
CAS#21498-08-8 (HCl)

Theoretical Analysis

MedKoo Cat#: 318158

Name: Lofexidine Hydrochloride

CAS#: 21498-08-8 (HCl)

Chemical Formula: C11H13Cl3N2O

Exact Mass: 0.0000

Molecular Weight: 295.59

Elemental Analysis: C, 44.70; H, 4.43; Cl, 35.98; N, 9.48; O, 5.41

Price and Availability

Size Price Availability Quantity
500mg USD 300.00 2 weeks
1g USD 550.00 2 weeks
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Related CAS #
21498-08-8 (HCl) 31036-80-3 (free base)
Synonym
Lofexidine Hydrochloride; Loxacor hydrochloride; MDL 14,042; MDL-14,042; MDL14,042; RMI-14042A; RMI14042A; RMI 14042A; BA 168; Lofetensin hydrochloride; Lucemyra.
IUPAC/Chemical Name
2-[1-(2,6-dichlorophenoxy)ethyl]-4,5-dihydro-1H-imidazole;hydrochloride
InChi Key
DWWHMKBNNNZGHF-UHFFFAOYSA-N
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
SMILES Code
CC(C1=NCCN1)OC2=C(C=CC=C2Cl)Cl.Cl
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, not in water
Shelf Life
>2 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
Product Data
Instruction
View handling instruction
Biological target:
Lofexidine (hydrochloride) is a selective α2-receptor agonist.
In vitro activity:
TBD
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMF 20.0 67.66
DMSO 65.0 219.90
Ethanol 30.0 101.49
PBS (pH 7.2) 10.0 33.83
Water 100.0 338.31
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 295.59 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.

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