Naloxonazine dihydrochloride
Based on 1 Customer Validation
Naloxonazine dihydrochloride is a specific μ-opioid receptor antagonist with an IC50 of 5.4 nM. Naloxonazine dihydrochloride also shows anti-leishmanial activity.
For research use only. We do not sell to patients.
- Purity: 98.1%
- CAS No.: 880759-65-9
- Formula: C38H44Cl2N4O6
- Molecular Weight:723.69
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
All Opioid Receptor Isoforms
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Biological Activity
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μ Opioid Receptor/MOR 5.4 nM (IC50) |
Naloxonazine is relatively stable in solution[2].
Naloxonazine (72 h) is active against the intracellular amastigote stage of Leishmania donovani with a half maximal inhibitory concentration (GI50) of 3.45 μM[3].
Naloxonazine (10 μM; 0-72 h) is active at early stages of Leishmania donovani infection[3].
Naloxonazine affects acidic compartments of the host cell which in turn limit L. donovani intracellular growth[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male ICR mice, methamphetamine (METH)-induced locomotor activity model[1]
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Dosage:20 mg/kg
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Administration:Intraperitoneal injection, once, 60 min before injecting saline (i.p.) or METH (1 mg/kg, i.p.)
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Result:Significantly attenuated the acute METH-induced increase in locomotor activity and phosphor-Thr75 DARPP-32 levels.
Chemical Information
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CAS No. 880759-65-9
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Appearance Solid
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Molecular Weight 723.69
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Formula C38H44Cl2N4O6
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Color White to off-white
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SMILES
O[C@@]([C@@]1([H])CC2=CC=C3O)(CC/4)[C@@]5(CCN1CC=C)C2=C3O[C@@]5([H])C4=N\N=C(CC[C@]67O)\[C@@]8([H])[C@]6(CCN(CC=C)[C@]7([H])CC9=CC=C%10O)C9=C%10O8.Cl.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H2O : ≥ 25 mg/mL (34.55 mM)
* "≥" means soluble, but saturation unknown.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Chien CC, et al. Naloxonazine, a specific mu-opioid receptor antagonist, attenuates the increment of locomotor activity induced by acute methamphetamine in mice. Toxicol Lett. 2012 Jul 7;212(1):61-5. [Content Brief]
[2]. Hahn EF, et al. Naloxonazine, a potent, long-lasting inhibitor of opiate binding sites. Life Sci. 1982 Sep 20-27;31(12-13):1385-8. [Content Brief]
[3]. De Muylder G, et al. Naloxonazine, an Amastigote-Specific Compound, Affects Leishmania Parasites through Modulation of Host-Encoded Functions. PLoS Negl Trop Dis. 2016 Dec 30;10(12):e0005234. [Content Brief]
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 (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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 1.3818 mL | 6.9090 mL | 13.8181 mL | 34.5452 mL |
| 5 mM | 0.2764 mL | 1.3818 mL | 2.7636 mL | 6.9090 mL | |
| 10 mM | 0.1382 mL | 0.6909 mL | 1.3818 mL | 3.4545 mL | |
| 15 mM | 0.0921 mL | 0.4606 mL | 0.9212 mL | 2.3030 mL | |
| 20 mM | 0.0691 mL | 0.3455 mL | 0.6909 mL | 1.7273 mL | |
| 25 mM | 0.0553 mL | 0.2764 mL | 0.5527 mL | 1.3818 mL | |
| 30 mM | 0.0461 mL | 0.2303 mL | 0.4606 mL | 1.1515 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.