Naltrexone

Cat. No.: HY-76711 Purity: 98.77%: FAQs
Data Sheet SDS COA Handling Instructions

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Naltrexone is an antagonist of Opioid receptor. Naltrexone inhibits cell proliferation in vivo. Naltrexone reduces tumor growth by interfering with cell signalling and modifying the immune system.

For research use only. We do not sell to patients.

Naltrexone Chemical Structure

CAS No. : 16590-41-3

Size	Stock	Quantity
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Based on 1 publication(s) in Google Scholar

Other Forms of Naltrexone:

Naltrexone-d₄ Get quote
Naltrexone metabolite 6β-Naltrexol hydrochloride Get quote
Naltrexone hydrochloride Get quote
Naltrexone (Standard) Get quote

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•Related Small Molecules:

•Related Proteins:

View All Opioid Receptor Isoform Specific Products:

View All Isoforms

μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

Biological Activity
Purity & Documentation
References
Customer Review

Description

Cellular Effect

Cell Line	Type	Value	Description	References
BV-2	IC₅₀	105.5 μM Compound: 31	Inhibition of LPS-induced NO production in mouse BV-2 microglia cells incubated for 24 hrs by 2,3-diaminonaphthalene assay Inhibition of LPS-induced NO production in mouse BV-2 microglia cells incubated for 24 hrs by 2,3-diaminonaphthalene assay	[PMID: 35307617]
CHO	EC₅₀	0.16 nM Compound: NTX	Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	[PMID: 25783191]
CHO	EC₅₀	0.16 nM Compound: NTX	Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs Agonist activity at mouse mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	[PMID: 23948248]
CHO	EC₅₀	0.81 nM Compound: NTX	Agonist activity at mouse KOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay Agonist activity at mouse KOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	[PMID: 25783191]
CHO	EC₅₀	0.81 nM Compound: NTX	Agonist activity at kappa opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs Agonist activity at kappa opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	[PMID: 24144240]
CHO	IC₅₀	0.95 nM Compound: NTX	Binding affinity to MOR Y210A mutant (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay Binding affinity to MOR Y210A mutant (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay	[PMID: 24055076]
CHO	IC₅₀	10.35 nM Compound: NTX	Binding affinity to MOR W318A mutant (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay Binding affinity to MOR W318A mutant (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay	[PMID: 24055076]
CHO	IC₅₀	15.5 nM Compound: NTX	Antagonist activity at human MOR expressed in CHO cells assessed as inhibition of DAMGO-induced increase in intracellular Ca2+ level incubated for 15 mins prior to DAMGO addition by microplate reader analysis Antagonist activity at human MOR expressed in CHO cells assessed as inhibition of DAMGO-induced increase in intracellular Ca2+ level incubated for 15 mins prior to DAMGO addition by microplate reader analysis	[PMID: 25783191]
CHO	IC₅₀	3.9 nM Compound: NTX	Binding affinity to wild type MOR (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay Binding affinity to wild type MOR (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay	[PMID: 24055076]
CHO	EC₅₀	4.4 nM Compound: NTX	Agonist activity at mouse DOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay Agonist activity at mouse DOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay	[PMID: 25783191]
CHO	EC₅₀	4.4 nM Compound: NTX	Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs Agonist activity at delta opioid receptor (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 1.5 hrs	[PMID: 24144240]
CHO	EC₅₀	5.44 nM Compound: NTX	Agonist activity at human recombinant delta opioid receptor expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay Agonist activity at human recombinant delta opioid receptor expressed in CHO cell membranes after 60 mins by [35S]GTPgammaS binding assay	[PMID: 24973818]
CHO	IC₅₀	8.9 nM Compound: NTX	Antagonist activity at human mu opioid receptor expressed in Gqi5 transfected CHO cells assessed as inhibition of DAMGO-stimulated Ca2+ influx preincubated for 15 mins followed by DAMGO challenge Antagonist activity at human mu opioid receptor expressed in Gqi5 transfected CHO cells assessed as inhibition of DAMGO-stimulated Ca2+ influx preincubated for 15 mins followed by DAMGO challenge	[PMID: 23682308]
HEK293	IC₅₀	157.51 μM Compound: Naltrexone	Inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysis Inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysis	[PMID: 31597043]

Molecular Weight

341.40

Formula

C₂₀H₂₃NO₄

CAS No.

16590-41-3

Appearance

Solid

Color

White to off-white

SMILES

OC1=CC=C2C3=C1O[C@](C(CC4)=O)([H])[C@@]3(CCN5CC6CC6)[C@]4(O)[C@@]5([H])C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 31 mg/mL (90.80 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.9291 mL	14.6456 mL	29.2912 mL
5 mM	0.5858 mL	2.9291 mL	5.8582 mL
10 mM	0.2929 mL	1.4646 mL	2.9291 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.94%

Select Batch:

Data Sheet (281 KB) SDS (735 KB)

COA (260 KB) HNMR (212 KB) RP-HPLC (340 KB) LCMS (266 KB)

Handling Instructions (2659 KB)

References

[1]. Couto RD, et al. Low Doses Naltrexone: The Potential Benefit Effects for its Use in Patients with Cancer. Curr Drug Res Rev. 2021;13(2):86-89. [Content Brief]

[2]. Lobmaier PP, et al. Naltrexone depot formulations for opioid and alcohol dependence: a systematic review. CNS Neurosci Ther. 2011 Dec;17(6):629-36. [Content Brief]

[3]. Mannelli P, Peindl KS, Wu LT. Pharmacological enhancement of naltrexone treatment for opioid dependence: a review. Subst Abuse Rehabil. 2011 Jun;2011(2):113-123. [Content Brief]

[4]. Swift R, Oslin DW, Alexander M, Forman R. Adherence monitoring in naltrexone pharmacotherapy trials: a systematic review. J Stud Alcohol Drugs. 2011 Nov;72(6):1012-8. [Content Brief]

[5]. Makowski CT, Gwinn KM, Hurren KM. Naltrexone/bupropion: an investigational combination for weight loss and maintenance. Obes Facts. 2011;4(6):489-94. [Content Brief]

[6]. Hulse GK. Improving Clinical Outcomes for Naltrexone as a Management of Problem Alcohol Use. Br J Clin Pharmacol. 2012 Sep 5. doi: 10.1111/j.1365-2125.2012.04452.x. [Content Brief]

[7]. Naltrexone

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.9291 mL	14.6456 mL	29.2912 mL	73.2279 mL
	5 mM	0.5858 mL	2.9291 mL	5.8582 mL	14.6456 mL
	10 mM	0.2929 mL	1.4646 mL	2.9291 mL	7.3228 mL
	15 mM	0.1953 mL	0.9764 mL	1.9527 mL	4.8819 mL
	20 mM	0.1465 mL	0.7323 mL	1.4646 mL	3.6614 mL
	25 mM	0.1172 mL	0.5858 mL	1.1716 mL	2.9291 mL
	30 mM	0.0976 mL	0.4882 mL	0.9764 mL	2.4409 mL
	40 mM	0.0732 mL	0.3661 mL	0.7323 mL	1.8307 mL
	50 mM	0.0586 mL	0.2929 mL	0.5858 mL	1.4646 mL
	60 mM	0.0488 mL	0.2441 mL	0.4882 mL	1.2205 mL
	80 mM	0.0366 mL	0.1831 mL	0.3661 mL	0.9153 mL

Naltrexone Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Naltrexone16590-41-3Opioid ReceptorOpioid receptor antagonistμ-opioid-receptorAnticancerInhibitorinhibitorinhibit

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Naltrexone

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Other Forms of Naltrexone:

Naltrexone Related Antibodies

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Biological Activity

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References

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Complete Stock Solution Preparation Table

Naltrexone Related Classifications

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