Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
Leishmania
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ln Vitro |
Namoline aloxonazine (0-50 μM, 24-72 h) has inhibitory efficacy against the amastigote stage of Leishmania donovani in cells with a maximum inhibitory concentration GI50 of 3.45 μM. For THP-1 host cells, the GI50 is 34 μM [1]. After 24 hours of treatment, naloxonazine (10 μM, 4-72 hours) can suppress the intracellular proliferation of parasites by 70%, and after 72 hours, it can decrease it by 95% [1]. The intracellular acidic compartment of the host cell is affected by naloxonazine (10 μM, 4 or 24-72 h), which also promotes the elevation of actin (ACTB) gene and protein expression levels and vATPase subunits (ATP6V0C and TCIRG1) [1].
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ln Vivo |
In male Wistar rats, naloxonazine (0–15 mg/kg, ip, 20 h) dramatically reduced the S+/CS+ associated responses (olfactory discriminative stimuli) by approximately 55%, from 14.63 to 6.82. The response rate dropped by 66%, from 9.00 to 3.00, under the (olfactory stimulus) S-/CS-stimulation condition, despite increased behavioral inhibition being seen [2].
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References |
[1]. Géraldine De Muylder, 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.
[2]. Roberto Ciccocioppo, et al. Effect of selective blockade of mu(1) or delta opioid receptors on reinstatement of alcohol-seeking behavior by drug-associated stimuli in rats. Neuropsychopharmacology. 2002 Sep;27(3):391-9. |
Molecular Formula |
C38H42N4O6
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Molecular Weight |
650.76
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CAS # |
82824-01-9
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Related CAS # |
Naloxonazine dihydrochloride;880759-65-9
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C=CCN1CC[C@]23C4/C(/CC[C@@]2(O)[C@H]1CC1=C3C(O4)=C(C=C1)O)=N/N=C1\CC[C@]2([C@@H]3N(CC[C@]42C2C(OC\14)=C(C=CC=2C3)O)CC=C)O
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HS Tariff Code |
2934.99.9001
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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)
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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
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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
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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 : PEG300 :Tween 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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.5367 mL | 7.6833 mL | 15.3666 mL | |
5 mM | 0.3073 mL | 1.5367 mL | 3.0733 mL | |
10 mM | 0.1537 mL | 0.7683 mL | 1.5367 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.
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.