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Naltrexone

Chemical Structure : Naltrexone

CAS No.: 16590-41-3

Naltrexone

Catalog No.: PC-45979Not For Human Use, Lab Use Only.

Naltrexone is a potent, competitive antagonist for μ, κ, δ, and σ-opioid receptors with Ki of 0.0825 nM, 0.509 nM, and 8.02 nM, for MOR, KOR, and DOR, respectively.

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Biological Activity

Naltrexone is a potent, competitive antagonist for μ, κ, δ, and σ-opioid receptors with Ki of 0.0825 nM, 0.509 nM, and 8.02 nM, for MOR, KOR, and DOR, respectively.
Naltrexone also inhibits IL-6 and TNFα production in human immune cell subsets following stimulation with ligands for intracellular TLRs.
Naltrexone is a TLR-4 antognist that inhibits LPS-induced TLR4 downstream NO production in microglia BV-2 cells (IC50=105 uM).

Physicochemical Properties

M.Wt 341.4009
Formula C20H23NO4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 31 mg/mL

Chemical Name/SMILES

Morphinan-6-one, 17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxy-, (5α)-

References

1. Codd EE, et al. J Pharmacol Exp Ther. 1995 Sep;274(3):1263-70.

2. Cant R, et al. Front Immunol. 2017 Jul 11;8:809.

3. Selfridge BR, et al. J Med Chem. 2015 Jun 25;58(12):5038-52.

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