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Purity: ≥98%
Nitazoxanide D4 (NTZ D4; NSC-697855 D4) is the deuterium labeled (deurated) form of Nitazoxanide, which is a synthetic nitrothiazolyl-salicylamide derivative and an antiprotozoal agent with IC50 for canine influenza virus ranges from 0.17 to 0.21 μM. Nitazoxanide was approved for treating human protozoan infections. Nitazoxanide reduces parasite growth in cell culture by more than 90% with little evidence of drug-associated cytotoxicity. Nitazoxanide is a new thiazolide antiparasitic agent that shows excellent in vitro activity against a wide variety of protozoa and helminths. Nitazoxanide and its metabolite tizoxanide are more active in vitro than metronidazole against G. intestinalis, E. histolytica and T. vaginalis.
| ln Vitro |
Nitazoxanide reduces parasite growth in cell culture by more than 90% with little evidence of drug-associated cytotoxicity. Nitazoxanide is a new thiazolide antiparasitic agent that shows excellent in vitro activity against a wide variety of protozoa and helminths. Nitazoxanide and its metabolite tizoxanide are more active in vitro than metronidazole against G. intestinalis, E. histolytica and T. vaginalis. Nitazoxanide exhibits potent inhibition of both HBV and HCV replication. Nitazoxanide potentiates the effect of subsequent treatment with Nitazoxanide plus IFN, but not Nitazoxanide plus 2CmeC, in HCV replicon-containing cells. Nitazoxanide induces reductions in several HBV proteins (HBsAg, HBeAg, HBcAg) produced by 2.2.15 cells, but does not affect HBV RNA transcription. Nitazoxanide exhibits IC50, and IC90 values of 0.017 and 0.776 mg/mL respectively, against E. histolytica, 0.004 and 0.067 mg/mL against G. intestinalis, and 0.034 and 2.046 mg/mL against T. vaginalis. Nitazoxanide is more toxic than metronidazole and albendazole against E. histolytica.
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| ln Vivo |
Nitazoxanide is partially effective at reducing the parasite burden in a gnotobiotic piglet diarrhea model when given orally for 11 days at 250 mg/kg/day but not at 125 mg/kg/day. Nitazoxanide induces a drug-related diarrhea in piglets that might have influenced its therapeutic efficacy.
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| References |
| Molecular Formula |
C12H9N3O5S
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| Molecular Weight |
311.31
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| Exact Mass |
311.051
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| CAS # |
1246819-17-9
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| Related CAS # |
Nitazoxanide;55981-09-4
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| PubChem CID |
71751033
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| Appearance |
White to off-white solid powder
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| LogP |
2.825
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
21
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| Complexity |
428
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[2H]C1=C(C(=C(C(=C1[2H])C(=O)NC2=NC=C(S2)[N+](=O)[O-])OC(=O)C)[2H])[2H]
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| InChi Key |
YQNQNVDNTFHQSW-QFFDRWTDSA-N
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| InChi Code |
InChI=1S/C12H9N3O5S/c1-7(16)20-9-5-3-2-4-8(9)11(17)14-12-13-6-10(21-12)15(18)19/h2-6H,1H3,(H,13,14,17)/i2D,3D,4D,5D
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| Chemical Name |
[2,3,4,5-tetradeuterio-6-[(5-nitro-1,3-thiazol-2-yl)carbamoyl]phenyl] acetate
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| Synonyms |
NTZ D4; NSC 697855 D4; NSC-697855; NSC697855 D4; Nitazoxanide D4, Alinia, Colufase, Daxon, NitazoxamideD4
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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) |
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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 | 3.2122 mL | 16.0612 mL | 32.1223 mL | |
| 5 mM | 0.6424 mL | 3.2122 mL | 6.4245 mL | |
| 10 mM | 0.3212 mL | 1.6061 mL | 3.2122 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.
Forward genetic screen for identification of NTZ resistant worm mutants.Mol Biochem Parasitol.2014 Jan;193(1):1-8. |
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Dose response curves ofC. elegansmutants resistant to other classes of drugs to NTZ in a six day lethality assay.Mol Biochem Parasitol.2014 Jan;193(1):1-8. |
Combination of NTZ with albendazole (ALB) and pyrantel (PYR).Mol Biochem Parasitol.2014 Jan;193(1):1-8. |
Ivermectin (IVM) susceptibility of the two NTZ resistant mutants identified in forward genetic screens at 44–45 hours.Mol Biochem Parasitol.2014 Jan;193(1):1-8. |
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Effect of NTZ onC. elegansN2 wild-type nematodes.Mol Biochem Parasitol.2014 Jan;193(1):1-8. |
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