Zanamivir [139110-80-8]

Cat# HY-13210-50mg

Size : 50mg

Brand : MedChemExpress


Zanamivir is an influenza viral neuraminidase inhibitor with IC50 values of 0.95 nM and 2.7 nM for influenza A and B, respectively.

For research use only. We do not sell to patients.

Zanamivir Chemical Structure

Zanamivir Chemical Structure

CAS No. : 139110-80-8

This product is a controlled substance and not for sale in your territory.

Based on 6 publication(s) in Google Scholar

Other Forms of Zanamivir:

  • Zanamivir (hydrate)(5:1) Get quote

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Description

Zanamivir is an influenza viral neuraminidase inhibitor with IC50 values of 0.95 nM and 2.7 nM for influenza A and B, respectively.

IC50 & Target

IC50: 0.95 nM (Influenza A); 2.7 nM (Influenza B)[1]

In Vitro

Zanamivir interacts with a group of amino acids in the active site of neuraminidase, which are conserved in all influenza A and B strains. Zanamivir blocks the action of neuraminidase, which prevents the cleavage of sialic acid on the cell receptors, thus preventing release and spread of the newly formed virions[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Zanamivir has a poor bioavailability in oral administration, with only 4–17% of the agent. Oral delivery of zanamivir has been a problem due to its strong hydrophilic nature that limits its transport across the intestinal epithelium. Permeation enhancers such as sodium cholate, hydroxypropyl β-cyclodextrin could be used with zanamivir to enhance the intestinal permeability[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

332.31

Formula

C12H20N4O7

CAS No.

139110-80-8

Appearance

Solid

Color

White to off-white

SMILES

NC(N[C@@H]1[C@H]([C@@](15)(OC(C(O)=O)=C1)[C@@H]([C@@H](CO)O)O)NC(C)=O)=N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

H2O : ≥ 33.33 mg/mL (100.30 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 9.09 mg/mL (27.35 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.92%

References
  • [1]. Gubareva LV, et al. Comparison of the activities of zanamivir, oseltamivir, and RWJ-270201 against clinical isolates ofinfluenza virus and neuraminidase inhibitor-resistant variants. Antimicrob Agents Chemother. 2001 Dec;45(12):3403-8.  [Content Brief]

    [2]. McKimm-Breschkin JL, et al. Management of influenza virus infections with neuraminidase inhibitors: detection, incidence, and implications of drug resistance. Treat Respir Med. 2005;4(2):107-16.  [Content Brief]

    [3]. Shanmugam S, et al. Zanamivir oral delivery: enhanced plasma and lung bioavailability in rats. Biomol Ther (Seoul). 2013 Mar;21(2):161-9.  [Content Brief]

Animal Administration
[3]

Rats: Formulations PO-SC (Zanamivir with SC for p.o.) and PO-C (Zanamivir control solution for p.o.) are administered orally at a Zanamivir dose of 10 mg/kg, and IV-R (reference Zanamivir saline solution for i.v.) is administered i.v. at a dose of 1 mg/kg to rats under conscious condition. Blood samples are collected prior to and at 0.5, 1, 2, 3, 4, 6, 8, and 24 hr after administration. At each sampling point, three rats from each group are sacrificed after blood collection to extract the lungs. The lungs are cleansed with saline after extraction of lungs from the rats through a chest incision. The lungs are then transferred into E-tube and stored in the freezer (-80°C) until analysis. Plasma samples are harvested by centrifugation at 1,500 × g for 10 min and stored at -20°C until analysis. The analysis of Zanamivir in both plasma and lungs is performed using before-mentioned LC-MS/MS method[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
  • [1]. Gubareva LV, et al. Comparison of the activities of zanamivir, oseltamivir, and RWJ-270201 against clinical isolates ofinfluenza virus and neuraminidase inhibitor-resistant variants. Antimicrob Agents Chemother. 2001 Dec;45(12):3403-8.  [Content Brief]

    [2]. McKimm-Breschkin JL, et al. Management of influenza virus infections with neuraminidase inhibitors: detection, incidence, and implications of drug resistance. Treat Respir Med. 2005;4(2):107-16.  [Content Brief]

    [3]. Shanmugam S, et al. Zanamivir oral delivery: enhanced plasma and lung bioavailability in rats. Biomol Ther (Seoul). 2013 Mar;21(2):161-9.  [Content Brief]

  • [1]. Gubareva LV, et al. Comparison of the activities of zanamivir, oseltamivir, and RWJ-270201 against clinical isolates ofinfluenza virus and neuraminidase inhibitor-resistant variants. Antimicrob Agents Chemother. 2001 Dec;45(12):3403-8.

    [2]. McKimm-Breschkin JL, et al. Management of influenza virus infections with neuraminidase inhibitors: detection, incidence, and implications of drug resistance. Treat Respir Med. 2005;4(2):107-16.

    [3]. Shanmugam S, et al. Zanamivir oral delivery: enhanced plasma and lung bioavailability in rats. Biomol Ther (Seoul). 2013 Mar;21(2):161-9.

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 3.0092 mL 15.0462 mL 30.0924 mL 75.2310 mL
5 mM 0.6018 mL 3.0092 mL 6.0185 mL 15.0462 mL
10 mM 0.3009 mL 1.5046 mL 3.0092 mL 7.5231 mL
15 mM 0.2006 mL 1.0031 mL 2.0062 mL 5.0154 mL
20 mM 0.1505 mL 0.7523 mL 1.5046 mL 3.7615 mL
25 mM 0.1204 mL 0.6018 mL 1.2037 mL 3.0092 mL
30 mM 0.1003 mL 0.5015 mL 1.0031 mL 2.5077 mL
40 mM 0.0752 mL 0.3762 mL 0.7523 mL 1.8808 mL
50 mM 0.0602 mL 0.3009 mL 0.6018 mL 1.5046 mL
60 mM 0.0502 mL 0.2508 mL 0.5015 mL 1.2538 mL
80 mM 0.0376 mL 0.1881 mL 0.3762 mL 0.9404 mL
100 mM 0.0301 mL 0.1505 mL 0.3009 mL 0.7523 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.

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Keywords:

Zanamivir139110-80-8Influenza VirusAntibioticInhibitorinhibitorinhibit

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