WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 563669
CAS#: 58895-64-0 (HCl)
Description: Nalmefene HCl is an antagonist of the opioid receptors.
MedKoo Cat#: 563669
Name: Nalmefene HCl
CAS#: 58895-64-0 (HCl)
Chemical Formula: C21H26ClNO3
Exact Mass: 375.1601
Molecular Weight: 375.893
Elemental Analysis: C, 67.10; H, 6.97; Cl, 9.43; N, 3.73; O, 12.77
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
| 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/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 37.59 | 100.0 | |
| Water | 37.59 | 100.0 |
The following data is based on the product molecular weight 375.893 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.
| 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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