Cat. No.: HY-17417

Naloxone hydrochloride

Name: Naloxone hydrochloride
Brand: MedChemExpress
SKU: HY-17417
Price: 50.00 USD
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Rating: 5 (8 reviews)

8 Cited Publications

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Based on 8 publication(s) in Google Scholar

Naloxone hydrochloride is an orally active opioid receptor antagonist. Naloxone hydrochloride attenuates spinal cord stimulation‑associated anti‑hyperalgesic effects, antagonizes physiologic effects of endogenous opioid peptides linked to central nervous system injury sequelae, functions as a pressor agent to induce modest elevations in mean arterial blood pressure, exerts neuroprotective effects to improve post‑traumatic neurologic motor function, blocks opioid receptor‑mediated amnesic pathways, enhances memory consolidation, reverses Adrenocorticotropic hormone (ACTH) (HY-106373)- and epinephrine‑induced amnesia, and potentiates the memory‑facilitatory effects of ACTH and epinephrine.

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

Purity: 99.96%
CAS No.: 357-08-4
Formula: C₁₉H₂₂ClNO₄
Molecular Weight:363.84

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Naloxone hydrochloride Chemical Structure

CAS No.: 357-08-4

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (8)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All Opioid Receptor Isoforms :

In Vitro

Naloxone (800 µg per tablet; 2 h annealing, 5 days freeze drying) hydrochloride forms freeze-dried buccal tablets that form a stable amorphous matrix that remains chemically and physically intact for 9 months at 4°C or 25°C^[4].
Naloxone (800 µg per tablet; up to 30 s) hydrochloride forms freeze-dried buccal tablets that achieve 90% disintegration in 4.8 seconds under buccal-relevant conditions (37°C, 0.7 mL phosphate buffer) and fully disintegrate within 30 s across all tested temperature and medium volume conditions^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Naloxone (10 mg/kg; i.p.; single dose) hydrochloride significantly inhibits the early SCS-induced reversal of neuropathic mechanical hypersensitivity in male Sprague Dawley rats, but has no effect on the incremental anti-hyperalgesic effect of late SCS^[1].
Naloxone (2.0 mg/kg; 1.7 mg/kg/h; i.v.; bolus over 60 seconds followed by constant infusion; 4 hours) hydrochloride significantly improves long-term neurologic motor recovery up to 4 weeks following moderate fluid-percussion traumatic brain injury in male Sprague-Dawley rats, with a median composite neurologic score of 18.5 at week 4^[2].
Naloxone (0.4 mg/kg; i.p.; single immediate post-training injection) hydrochloride produces significant memory facilitation in male Wistar rats trained on task 1 and 2, and reverses the amnesic effects of post-training ACTH and epinephrine administration^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Sprague Dawley (adult male, 200-250 g, neuropathic pain model via partial sciatic nerve ligation and epidural monopolar electrode implantation at spinal segments T12/13)^[1]
Dosage:

10 mg/kg
Administration:

i.p.; single dose
Result:

Decreased the ipsilateral:contralateral paw withdrawal threshold ratio after SCS1.
Exerted no discernible effect on the anti-hyperalgesic effect induced by SCS2.

Animal Model:

Sprague-Dawley (male, moderate severity lateral fluid-percussion traumatic brain injury induced via 2.4 to 2.5 atmosphere pressure pulse)^[2]
Dosage:

2.0 mg/kg (bolus); 1.7 mg/kg/h (infusion)
Administration:

i.v.; bolus over 60 seconds followed by constant infusion; 4 hours
Result:

Caused a modest, nonsignificant increase in mean arterial blood pressure during 4-hour postinjury monitoring period.
Showed no significant changes to arterial blood gases, pH, or brain temperature.
Exhibited no significant improvement in composite neurologic motor scores at 24 hours postinjury.
Achieved a significant improvement in median composite neurologic motor scores at 1 week postinjury.
Reached a median composite neurologic motor score of 18.5 out of maximum 20 by week 4.
Resulted in 100% survival rate over the 4-week study period.

Animal Model:

Wistar rats (male, age 51-69 days, weight 140-200 g, step-down inhibitory avoidance task 1 training)^[3]
Dosage:

0.4 mg/kg
Administration:

i.p.; single immediate post-training injection
Result:

Produced a median (mean) training-test step-down latency difference of 180.00 sec.
Produced a median (mean) training-test step-down latency difference of 180.00 (144.45) sec when co-administered with 2.0 μg/kg ACTH_1-24, reversing the amnesic effect of ACTH alone and showing a significant difference from naloxone alone.
Produced a median (mean) training-test step-down latency difference of 180.00 (134.98) sec when co-administered with 50.0 μg/kg epinephrine HC1, reversing the amnesic effect of epinephrine alone and showing a significant difference from naloxone alone.

Animal Model:

Wistar rats (male, age 51-69 days, weight 140-200 g, step-down inhibitory avoidance task 2 training)^[3]
Dosage:

0.4 mg/kg
Administration:

i.p.; single immediate post-training injection
Result:

Produced a median (mean) training-test step-down latency difference of 24.13 (56.18) sec, showing significant memory facilitation compared to saline controls.
Produced a median (mean) training-test step-down latency difference of 105.07 (113.65) sec when co-administered with 2.0 μg/kg ACTH_1-24, potentiating the facilitatory effect of ACTH alone and showing a significant difference from naloxone alone .
Produced a median (mean) training-test step-down latency difference of 81.85 (96.86) sec when co-administered with 50.0 μg/kg epinephrine HC1, potentiating the facilitatory effect of epinephrine alone and showing a significant difference from naloxone alone.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 357-08-4
Appearance Solid
Molecular Weight 363.84
Formula C₁₉H₂₂ClNO₄
Color White to off-white
SMILES

OC1=C(O2)C([C@]([C@]2([H])C(CC3)=O)(CCN4CC=C)[C@]3(O)[C@H]4C5)=C5C=C1.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (8)

All OthersCell Proliferation/Viability Assay

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Journal Impact Factor

Nature

Structural snapshots capture nucleotide release at the μ-opioid receptor. [Abstract]

2025 Dec;648(8094):755-763. PMID: 41193810
Nat Methods

Single-molecule localization and diffusivity microscopy reveals dynamic biomolecular organization in living cells. [Abstract]

2026 May;23(5):1011-1023. PMID: 42050111
Nat Commun

Neuropeptide Y neurons mediate opioid-induced itch by disinhibiting GRP-GRPR microcircuits in the spinal cord. [Abstract]

2025 Aug 1;16(1):7074. PMID: 40750771

Naloxone hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Aug 1;16(1):7074. [Abstract]

Heatmaps shows the calcium signals within the 10-25 min after drugs injection (i.t., 0.3 nmol Morphine, 10 nmol Naloxone + 0.3 nmol Morphine, and 10 μg NPY + 0.3 nmol Morphine), n = 5 mice per group.
Cell Rep

Morphine and Naloxone Facilitate Neural Stem Cells Proliferation via a TET1-Dependent and Receptor-Independent Pathway. [Abstract]

2020 Mar 17;30(11):3625-3631.e6. PMID: 32187535

Naloxone hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Rep. 2020 Mar 17;30(11):3625-3631.e6. [Abstract]

NSCs were treated with different concentrations of Naloxone, Morphine, Naloxone and Morphine (Mor+Nal, 1:1), or Nal-M. Cell numbers were determined on day 3.

Naloxone hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Rep. 2020 Mar 17;30(11):3625-3631.e6. [Abstract]

Neural stem cells (NSCs) were treated with 1 μM Naloxone or Morphine. The contents of 5mC and 5hmC in NSCs (day 3) were determined by high-spot Western blot assay.
Br J Pharmacol

Semax peptide targets the μ opioid receptor gene Oprm1 to promote deubiquitination and functional recovery after spinal cord injury in female mice. [Abstract]

2025 Jul 21. PMID: 40692165
J Med Chem

2026 Mar 5;69(6):6508-6527.
Eur J Pain

Endocannabinoid activation of CB1 receptors contributes to long-lasting reversal of neuropathic pain by repetitive spinal cord stimulation. [Abstract]

2017 May;21(5):804-814. PMID: 28107590

Naloxone hydrochloride purchased from MedChemExpress. Usage Cited in: Eur J Pain. 2017 May;21(5):804-814. [Abstract]

The SCS1 (early SCS)-mediated increase in the ipsilateral:contralateral PWT ratio (compared to pre-SCS) is significantly reduced by the opioid receptor antagonist, Naloxone, which is administered 10 min before SCS1.
bioRxiv

2026 Jun 3.

Solvent & Solubility

In Vitro:

H₂O : 62.5 mg/mL (171.78 mM; Need ultrasonic)

DMSO : ≥ 30 mg/mL (82.45 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7485 mL

13.7423 mL

27.4846 mL

5 mM

0.5497 mL

2.7485 mL

5.4969 mL

10 mM

0.2748 mL

1.3742 mL

2.7485 mL

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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

Protocol 1

Naloxone is made up in a vehicle of 2% dimethylformamide (aqueous)^[4].

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (307 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Sun L, et al. Endocannabinoid activation of CB receptors contributes to long-lasting reversal of neuropathic pain by repetitive spinal cord stimulation. European journal of pain (London, England). 2017 May;21(5):804-814. [Content Brief]

[2]. McIntosh TK, et al. Beneficial effect of the nonselective opiate antagonist naloxone hydrochloride and the thyrotropin-releasing hormone (TRH) analog YM-14673 on long-term neurobehavioral outcome following experimental brain injury in the rat. J Neurotrauma. 1993 Winter;10(4):373-84.
[Content Brief]

[3]. Izquierdo I, et al. Effect of ACTH, epinephrine, beta-endorphin, naloxone, and of the combination of naloxone or beta-endorphin with ACTH or epinephrine on memory consolidation. Psychoneuroendocrinology. 1983;8(1):81-7. [Content Brief]

[4]. Alqurshi A, et al. Amorphous Formulation and in Vitro Performance Testing of Instantly Disintegrating Buccal Tablets for the Emergency Delivery of Naloxone. Molecular pharmaceutics. 2016 May 02;13(5):1688-98.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / H₂O	1 mM	2.7485 mL	13.7423 mL	27.4846 mL	68.7115 mL
	5 mM	0.5497 mL	2.7485 mL	5.4969 mL	13.7423 mL
	10 mM	0.2748 mL	1.3742 mL	2.7485 mL	6.8712 mL
	15 mM	0.1832 mL	0.9162 mL	1.8323 mL	4.5808 mL
	20 mM	0.1374 mL	0.6871 mL	1.3742 mL	3.4356 mL
	25 mM	0.1099 mL	0.5497 mL	1.0994 mL	2.7485 mL
	30 mM	0.0916 mL	0.4581 mL	0.9162 mL	2.2904 mL
	40 mM	0.0687 mL	0.3436 mL	0.6871 mL	1.7178 mL
	50 mM	0.0550 mL	0.2748 mL	0.5497 mL	1.3742 mL
	60 mM	0.0458 mL	0.2290 mL	0.4581 mL	1.1452 mL
	80 mM	0.0344 mL	0.1718 mL	0.3436 mL	0.8589 mL
H₂O	100 mM	0.0275 mL	0.1374 mL	0.2748 mL	0.6871 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Bioz

Keywords

Naloxone hydrochloride

8 Cited Publications

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