Nalmefene HCl
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MedKoo CAT#: 563669

CAS#: 58895-64-0 (HCl)

Description: Nalmefene HCl is an antagonist of the opioid receptors.


Chemical Structure

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Nalmefene HCl
CAS# 58895-64-0 (HCl)

Theoretical Analysis

MedKoo Cat#: 563669
Name: Nalmefene HCl
CAS#: 58895-64-0 (HCl)
Chemical Formula: C21H26ClNO3
Exact Mass: 375.16
Molecular Weight: 375.893
Elemental Analysis: C, 67.10; H, 6.97; Cl, 9.43; N, 3.73; O, 12.77

Price and Availability

Size Price Availability Quantity
50mg USD 450 2 Weeks
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Related CAS #: 55096-26-9 (free base)   58895-64-0 (HCl)   1228646-70-5 (HCl dihydrate)   1228646-72-7 (HCl hydrate),  

Synonym: Nalmefene Hydrochloride; Nalmefene HCl;

IUPAC/Chemical Name: 17-(Cyclopropylmethyl)-4,5alpha-epoxy-6-methylenemorphinan-3,14-diol hydrochloride

InChi Key: GYWMRGWFQPSQLK-WFYNUGCWSA-N

InChi Code: InChI=1S/C21H25NO3.ClH/c1-12-6-7-21(24)16-10-14-4-5-15(23)18-17(14)20(21,19(12)25-18)8-9-22(16)11-13-2-3-13;/h4-5,13,16,19,23-24H,1-3,6-11H2;1H/t16-,19-,20+,21-;/m1./s1

SMILES Code: OC(C1=C2[C@@]34[C@@H]5O1)=CC=C2C[C@@H](N(CC6CC6)CC4)[C@]3(O)CCC5=C.[H]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

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: Nalmefene HCl is an antagonist of the opioid receptors.
In vitro activity: This study investigated whether nalmefene, an opioid receptor inhibitor, could inhibit CT26 colon cancer cell growth through influencing cell glycolysis. CCK8 and transwell migration assays showed that nalmefene inhibited CT26 cells viability and migration in a concentration-dependent manner. In conclusion, the anti-tumor effect of nalmefene may be achieved by inhibiting opioid receptor and down-regulating calmodulin expression and CaMK II phosphorylation, thus inhibiting AKT-GSK-3β pathway and the glycolysis of CT26 cells. Reference: Acta Biochim Biophys Sin (Shanghai). 2018 Feb 1;50(2):156-163. https://pubmed.ncbi.nlm.nih.gov/29267844/
In vivo activity: This study examined the effects of NMF (nalmefene) pretreatment on chronic daily extended access (4h) cocaine intravenous self-administration (IVSA) in adult male C57Bl/6J mice. Acute pretreatment of 1 mg/kg NMF significantly potentiated cocaine motivation as measured by progressive ratio breakpoint. Reference: Neuropharmacology. 2021 Jul 1;192:108590. https://pubmed.ncbi.nlm.nih.gov/33974940/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 37.6 100.00
Water 37.6 100.00

Preparing Stock Solutions

The following data is based on the product molecular weight 375.89 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: 1. Wu Q, Chen X, Wang J, Sun P, Weng M, Chen W, Sun Z, Zhu M, Miao C. Nalmefene attenuates malignant potential in colorectal cancer cell via inhibition of opioid receptor. Acta Biochim Biophys Sin (Shanghai). 2018 Feb 1;50(2):156-163. doi: 10.1093/abbs/gmx131. PMID: 29267844. 2. Windisch KA, Morochnik M, Reed B, Kreek MJ. Nalmefene, a mu opioid receptor antagonist/kappa opioid receptor partial agonist, potentiates cocaine motivation but not intake with extended access self-administration in adult male mice. Neuropharmacology. 2021 Jul 1;192:108590. doi: 10.1016/j.neuropharm.2021.108590. Epub 2021 May 8. PMID: 33974940. 3. Browne CA, Smith T, Lucki I. Behavioral effects of the kappa opioid receptor partial agonist nalmefene in tests relevant to depression. Eur J Pharmacol. 2020 Apr 5;872:172948. doi: 10.1016/j.ejphar.2020.172948. Epub 2020 Jan 25. PMID: 31991139.
In vitro protocol: 1. Wu Q, Chen X, Wang J, Sun P, Weng M, Chen W, Sun Z, Zhu M, Miao C. Nalmefene attenuates malignant potential in colorectal cancer cell via inhibition of opioid receptor. Acta Biochim Biophys Sin (Shanghai). 2018 Feb 1;50(2):156-163. doi: 10.1093/abbs/gmx131. PMID: 29267844.
In vivo protocol: 1. Windisch KA, Morochnik M, Reed B, Kreek MJ. Nalmefene, a mu opioid receptor antagonist/kappa opioid receptor partial agonist, potentiates cocaine motivation but not intake with extended access self-administration in adult male mice. Neuropharmacology. 2021 Jul 1;192:108590. doi: 10.1016/j.neuropharm.2021.108590. Epub 2021 May 8. PMID: 33974940. 2. Browne CA, Smith T, Lucki I. Behavioral effects of the kappa opioid receptor partial agonist nalmefene in tests relevant to depression. Eur J Pharmacol. 2020 Apr 5;872:172948. doi: 10.1016/j.ejphar.2020.172948. Epub 2020 Jan 25. PMID: 31991139.

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1: Seidi S, Yamini Y, Rezazadeh M, Esrafili A. Low-voltage electrically-enhanced microextraction as a novel technique for simultaneous extraction of acidic and basic drugs from biological fluids. J Chromatogr A. 2012 Jun 22;1243:6-13. doi: 10.1016/j.chroma.2012.04.050. Epub 2012 Apr 26. PubMed PMID: 22575744.

2: Mason BJ, Ritvo EC, Morgan RO, Salvato FR, Goldberg G, Welch B, Mantero-Atienza E. A double-blind, placebo-controlled pilot study to evaluate the efficacy and safety of oral nalmefene HCl for alcohol dependence. Alcohol Clin Exp Res. 1994 Oct;18(5):1162-7. PubMed PMID: 7847600.

3: Simpkins JW, Swager D, Millard WJ. Evaluation of the sites of opioid influence on anterior pituitary hormone secretion using a quaternary opiate antagonist. Neuroendocrinology. 1991 Oct;54(4):384-90. PubMed PMID: 1661859.

4: Fudala PJ, Johnson RE, Heishman SJ, Cone EJ, Henningfield JE. A dose run-up and safety evaluation of nalmefene HCl in human volunteers. NIDA Res Monogr. 1989;95:451-2. PubMed PMID: 2641028.

5: Simpkins JW, Smulkowski M, Dixon R, Tuttle R. Evidence for the delivery of narcotic antagonists to the colon as their glucuronide conjugates. J Pharmacol Exp Ther. 1988 Jan;244(1):195-205. PubMed PMID: 3335997.

6: Dixon R, Gentile J, Hsu HB, Hsiao J, Howes J, Garg D, Weidler D. Nalmefene: safety and kinetics after single and multiple oral doses of a new opioid antagonist. J Clin Pharmacol. 1987 Mar;27(3):233-9. PubMed PMID: 3680580.