| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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Zanamivir (GR-121167X; GG-167; Relenza) is a novel and potent neuraminidase inhibitor with antiviral activity against influenza. It inhibits influenza with IC50 values of 0.95 nM and 2.7 nM for influenza A and B, respectively. It can be used in the treatment and prophylaxis of influenza caused by influenza A and B viruses. Zanamivir acts by binding to the active site of the neuraminidase protein, rendering the influenza virus unable to escape its host cell and infect others. It is also an inhibitor of influenza virus replication in vitro and in vivo.
| Targets |
Influenza A(IC50= 0.95 nM);Influenza B(IC50= 2.7 nM)
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|---|---|
| ln Vitro |
Zanamivir (GR-121167X; GG-167; Relenza) interacts with a group of amino acids in the active site of neuraminidase, which are conserved in all influenza A and B strains.By inhibiting neuraminidase's ability to cleave sialic acid on cell receptors, zanamivir stops the release and dissemination of newly formed virions[2].
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| ln Vivo |
Zanamivir has a poor bioavailability in oral administration, with only 4–17% of the agent. Because of its strong hydrophilic nature, which restricts its transport across the intestinal epithelium, oral delivery of zanamivir has proven to be problematic. When combined with zanamivir, permeability enhancers like sodium cholate and hydroxypropyl β-cyclodextrin can improve intestinal permeability[3].
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| Animal Protocol |
Rats
Combinations Rats kept conscious are given IV-R (reference Zanamivir saline solution for intravenous injection) at a dose of 1 mg/kg.PO-SC (Zanamivir with SC for p.o.) and PO-C (Zanamivir control solution for p.o.) are given oral Zanamivir doses of 10 mg/kg. Before, at 0.5, 1, 2, 3, 4, 6, 8, and 24 hours after administration, blood samples are taken. Three rats from each group are sacrificed at each sampling point to remove the lungs following blood collection.After the rats' lungs are removed through a chest incision, the lungs are cleaned with saline. After that, the lungs are placed in an E-tube and kept in a freezer at -80°C until they are examined. After being centrifuged at 1,500 × g for 10 minutes, plasma samples are collected and kept at -20°C until analysis. Zanamivir is analyzed using the previously stated LC-MS/MS method in both plasma and lungs[3]. |
| References |
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| Molecular Formula |
C12H20N4O7
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|---|---|
| Molecular Weight |
332.313
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| Exact Mass |
332.1332
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| Elemental Analysis |
C, 43.37; H, 6.07; N, 16.86; O, 33.70
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| CAS # |
139110-80-8
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| Related CAS # |
Zanamivir (hydrate)(5:1);171094-50-1
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| Appearance |
Solid powder
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| SMILES |
O=C(C1=C[C@H](/N=C(N)\N)[C@@H](NC(C)=O)[C@H]([C@H](O)[C@H](O)CO)O1)O
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| InChi Key |
ARAIBEBZBOPLMB-UFGQHTETSA-N
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| InChi Code |
InChI=1S/C12H20N4O7/c1-4(18)15-8-5(16-12(13)14)2-7(11(21)22)23-10(8)9(20)6(19)3-17/h2,5-6,8-10,17,19-20H,3H2,1H3,(H,15,18)(H,21,22)(H4,13,14,16)/t5-,6+,8+,9+,10+/m0/s1
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| Chemical Name |
(2R,3R,4S)-3-acetamido-4-(diaminomethylideneamino)-2-[(1R,2R)-1,2,3-trihydroxypropyl]-3,4-dihydro-2H-pyran-6-carboxylic acid
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| Synonyms |
Zanamivir; GR-121167X; GG167; GR121167X; GG-167; GR 121167X; GG 167; trade name Relenza.
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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) |
H2O : 33.33~36 mg/mL (~100.30 mM)
DMSO : ~66 mg/mL ( ~198.6 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 9.09 mg/mL (27.35 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0092 mL | 15.0462 mL | 30.0924 mL | |
| 5 mM | 0.6018 mL | 3.0092 mL | 6.0185 mL | |
| 10 mM | 0.3009 mL | 1.5046 mL | 3.0092 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.
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