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Naloxone HCl Dihydrate

Alias: Naloxone HCl 2H2O; Naloxone HCl Dihydrate; Naloxone Hydrochloride Dihydrate
Cat No.:V22291 Purity: ≥98%
Naloxone HCl Dihydrate is a novel and potent opiate antagonist
Naloxone HCl Dihydrate
Naloxone HCl Dihydrate Chemical Structure CAS No.: 51481-60-8
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price
500mg
1g
Other Sizes

Other Forms of Naloxone HCl Dihydrate:

  • Naloxone
  • Naloxone HCl
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
Naloxone HCl Dihydrate is a novel and potent opiate antagonist
Biological Activity I Assay Protocols (From Reference)
Additional Infomation
See also: ...View more...
Drug Indications
Nyxoid is indicated for immediate use as an emergency treatment in both non-medical and medical settings for the treatment of known or suspected opioid overdose of respiratory and/or central nervous system depression. Nyxoid is indicated for use in adults and adolescents aged 14 years and older. Nyxoid is not a substitute for emergency medical care.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H26CLNO6
Molecular Weight
399.86
Exact Mass
399.144
CAS #
51481-60-8
Related CAS #
465-65-6;51481-60-8 (HCl hydrate);357-08-4 (HCl);
PubChem CID
20112022
Appearance
Typically exists as solid at room temperature
Melting Point
182 °C (dec.)(lit.)
Flash Point
288.4ºC
LogP
1.912
Hydrogen Bond Donor Count
5
Hydrogen Bond Acceptor Count
7
Rotatable Bond Count
2
Heavy Atom Count
27
Complexity
594
Defined Atom Stereocenter Count
4
SMILES
[C@@]123CCN(CC=C)[C@@H]4CC5C=CC(O)=C(O[C@H]1C(=O)CC[C@]24O)C3=5.Cl.O.O
InChi Key
TXMZWEASFRBVKY-IOQDSZRYSA-N
InChi Code
InChI=1S/C19H21NO4.ClH.2H2O/c1-2-8-20-9-7-18-15-11-3-4-12(21)16(15)24-17(18)13(22)5-6-19(18,23)14(20)10-11;;;/h2-4,14,17,21,23H,1,5-10H2;1H;2*1H2/t14-,17+,18+,19-;;;/m1.../s1
Chemical Name
(4R,4aS,7aR,12bS)-4a,9-dihydroxy-3-prop-2-enyl-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-one;dihydrate;hydrochloride
Synonyms
Naloxone HCl 2H2O; Naloxone HCl Dihydrate; Naloxone Hydrochloride Dihydrate
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
Solubility (In Vivo)
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)


Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.5009 mL 12.5044 mL 25.0088 mL
5 mM 0.5002 mL 2.5009 mL 5.0018 mL
10 mM 0.2501 mL 1.2504 mL 2.5009 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
A Phase 2 Safety, Tolerability, PK, and Efficacy Study of CS-1103 Following Fentanyl Challenge With Naloxone Blockade
CTID: NCT07459166
Phase: Phase 2
Status: Recruiting
Date: 2026-05-29
Symptom-Inhibited Naloxone Induction (SINI) for Buprenorphine Initiation: A Feasibility Trial
CTID: NCT07439549
Phase: Phase 4
Status: Recruiting
Date: 2026-05-01
Pharmacodynamic Evaluation of Intranasal Nalmefene
CTID: NCT04828005
Phase: Phase 1
Status: Completed
Date: 2025-07-14
The Effect of Chronic Pain on Delay Discounting in Methadone Patients
CTID: NCT04473950
Phase: Phase 1
Status: Terminated
Date: 2025-03-26
Reversal of Opioid-induced Respiratory Depression With Opioid Antagonists
CTID: NCT05338632
Phase: Phase 1
Status: Recruiting
Date: 2025-01-31
A Phase 4 Clinical Study to Investigate the Efficacy and Safety of Naloxone HCI IV in Patients With Stroke
CTID: NCT05301712
Phase: Phase 4
Status: Completed
Date: 2023-08-14
Clinical Outcomes From Nalmefene
CTID: NCT05808881
Phase: Phase 4
Status: Withdrawn
Date: 2023-07-12
Topical Naloxone to Diagnose Ocular Pain
CTID: NCT04454281
Phase: Phase 1
Status: Completed
Date: 2022-11-08
Treatment of Gambling Disorder With Fast Acting Opiate Antagonist, Naloxone Nasal Spray
CTID: NCT03223896
Phase: Phase 2
Status: Completed
Date: 2019-09-12
Effects of Intranasal Naloxone on Gambling Urges and Craving in Gambling Disorder
CTID: NCT03430180
Phase: Phase 2
Status: Unknown status
Date: 2019-07-16
Naloxone in Treating Constipation in Patients Who Are Receiving Opioids for Chronic Pain
CTID: NCT00020605
Phase: Phase 3
Status: Unknown status
Date: 2018-12-13
Double-blind, placebo-controlled randomised study on the efficacy of naloxone nasal spray for the treatment of gambling disorder
EudraCT: 2017-001946-93
Phase: Phase 2
Status: Completed
Date: 2017-10-31
Randomised, double-blind, placebo controlled trial evaluating the effects of naloxone hydrochloride nasal spray on eating behaviours in bulimia nervosa
EudraCT: 2016-003107-65
Phase: Phase 2
Status: Completed
Date: 2017-01-11
Rahapeliriippuvuuden hoitaminen nopeasti vaikuttavalla opioidinsalpaajalla (naloksonia sisältävä nenäsumute), tutkijalähtöinen tutkimus
EudraCT: 2016-001828-56
Phase: Phase 2
Status: Completed
Date: 2016-12-09
Open-label, uncontrolled trial to evaluate pharmacokinetics of naloxone in children from 4 to less than 18 years of age with opioid-induced constipation
EudraCT: 2015-002310-72
Phase: Phase 2
Status: Prematurely Ended, Temporarily Halted, Completed
Date: 2016-03-29
The NAPRESSIM trial.
EudraCT: 2015-003504-22
Phase: Phase 4
Status: Completed
Date: 2015-10-09
Single Intravenous Bolus Dose Safety and Opioid Reversal Pharmacodynamic Study of Naloxone in Healthy Opioid-Exposed Volunteers
CTID: Not Applicable
Phase: Phase 1
Status: Completed
Date: 1967
Phase 1 Comparative Pharmacokinetic Trial of IV, Intramuscular, Nasal and Subcutaneous Naloxone in Healthy Subjects
CTID: NCT01982549
Phase: Phase 1
Status: Completed
Date: 2013-12-10
QT/QTc Cardiac Safety Phase 1 Study of Supratherapeutic Doses of Intravenous Naloxone in Healthy Adults
CTID: NCT02614079
Phase: Phase 1
Status: Completed
Date: 2015-11-23
Randomized Double-Blind Phase 2 Trial of Low-Dose Oral Naloxone to Prevent Opioid-Induced Constipation in Chronic Pain Patients
CTID: NCT00432315
Phase: Phase 2
Status: Completed
Date: 2007-09-18
Multicenter Phase 2 Trial of Intranasal Naloxone for Prehospital Opioid Overdose Rescue by Lay Bystanders
CTID: NCT01516284
Phase: Phase 2
Status: Completed
Date: 2012-05-21
Pivotal Multicenter Double-Blind Phase 3 Trial of Oral Naloxone for Opioid-Induced Bowel Dysfunction in Chronic Non-Malignant Pain
CTID: NCT01094640
Phase: Phase 3
Status: Completed
Date: 2010-03-16
Open-Label Long-Term Phase 3 Extension Safety Study of Oral Naloxone in Patients With Opioid-Related Constipation
CTID: NCT01124712
Phase: Phase 3
Status: Completed
Date: 2011-01-05
Multicenter Randomized Phase 3 Trial Comparing Intranasal Naloxone Versus Injectable Naloxone for Out-of-Hospital Opioid Overdose Reversal
CTID: NCT02354117
Phase: Phase 3
Status: Completed
Date: 2014-12-08
Nationwide Post-Marketing Phase 4 Observational Safety Study of Take-Home Naloxone Distribution Programs for Opioid Overdose Prevention
CTID: NCT03446011
Phase: Phase 4
Status: Completed
Date: 2018-04-12
Phase 4 Comparative Effectiveness Study of Naloxone Auto-Injector vs Nasal Spray Administered by Untrained Lay Rescuers
CTID: NCT04123478
Phase: Phase 4
Status: Active, not recruiting
Date: 2020-06-30
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