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> Clevudine [163252-36-6]

Clevudine [163252-36-6]

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Size : 100mg

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Clevudine (L-FMAU), a nucleoside analog of the unnatural L-configuration, has potent anti-HBV activity with long half-life, low toxicity. Clevudine is a non-competitive inhibitor that is not incorporated into the viral DNA but rather binds to the polymerase. Clevudine is active against cowpox virus respiratory infection in mice.

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Clevudine Chemical Structure

Clevudine Chemical Structure

CAS No. : 163252-36-6

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

Description

Clevudine (L-FMAU), a nucleoside analog of the unnatural L-configuration, has potent anti-HBV activity with long half-life, low toxicity. Clevudine is a non-competitive inhibitor that is not incorporated into the viral DNA but rather binds to the polymerase. Clevudine is active against cowpox virus respiratory infection in mice[1][2][3].

In Vitro

Clevudine (L-FMAU) shows some activity against Epstein-Barr virus[2].

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

Clevudine Related Antibodies
Essai clinique
Masse moléculaire

260.22

Formule

C10H13FN2O5
CAS No.

163252-36-6
Appearance

Solid

Color

White to off-white

SMILES

O[C@@H]1[C@@H](F)[C@@H](N2C(NC(C(C)=C2)=O)=O)O[C@H]1CO
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvant et solubilité
In Vitro: 

DMSO : 100 mg/mL (384.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 50 mg/mL (192.15 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.8429 mL 19.2145 mL 38.4290 mL
5 mM 0.7686 mL 3.8429 mL 7.6858 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, 6 months; -20°C, 1 month. 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.

  • Calculateur de molarité

  • Calculateur de dilution

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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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).
Pureté et documentation

Purity: 99.93%

COA (253 KB) LCMS (263 KB)

Instruction de manipulation (2659 KB)
Références

  • [1]. Asselah T, et al. Clevudine: a promising therapy for the treatment of chronic hepatitis B. Expert Opin Investig Drugs. 2008;17(12):1963-1974.  [Content Brief]

    [2]. Yoo BC, et al. Clevudine is highly efficacious in hepatitis B e antigen-negative chronic hepatitis B with durable off-therapy viral suppression. Hepatology. 2007;46(4):1041-1048.  [Content Brief]

    [3]. Smee DF, et, al. Progress in the discovery of compounds inhibiting orthopoxviruses in animal models. Antivir Chem Chemother. 2008;19(3):115-24.  [Content Brief]

  • [1]. Asselah T, et al. Clevudine: a promising therapy for the treatment of chronic hepatitis B. Expert Opin Investig Drugs. 2008;17(12):1963-1974.

    [2]. Yoo BC, et al. Clevudine is highly efficacious in hepatitis B e antigen-negative chronic hepatitis B with durable off-therapy viral suppression. Hepatology. 2007;46(4):1041-1048.

    [3]. Smee DF, et, al. Progress in the discovery of compounds inhibiting orthopoxviruses in animal models. Antivir Chem Chemother. 2008;19(3):115-24.

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. 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 / DMSO 1 mM 3.8429 mL 19.2145 mL 38.4290 mL 96.0726 mL
5 mM 0.7686 mL 3.8429 mL 7.6858 mL 19.2145 mL
10 mM 0.3843 mL 1.9215 mL 3.8429 mL 9.6073 mL
15 mM 0.2562 mL 1.2810 mL 2.5619 mL 6.4048 mL
20 mM 0.1921 mL 0.9607 mL 1.9215 mL 4.8036 mL
25 mM 0.1537 mL 0.7686 mL 1.5372 mL 3.8429 mL
30 mM 0.1281 mL 0.6405 mL 1.2810 mL 3.2024 mL
40 mM 0.0961 mL 0.4804 mL 0.9607 mL 2.4018 mL
50 mM 0.0769 mL 0.3843 mL 0.7686 mL 1.9215 mL
60 mM 0.0640 mL 0.3202 mL 0.6405 mL 1.6012 mL
80 mM 0.0480 mL 0.2402 mL 0.4804 mL 1.2009 mL
100 mM 0.0384 mL 0.1921 mL 0.3843 mL 0.9607 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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Clevudine Related Classifications

  • Infection
  • Anti-infection Cell Cycle/DNA Damage
  • HBV DNA/RNA Synthesis Orthopoxvirus
Help & FAQs

Keywords:

Clevudine163252-36-6L-FMAUHBVDNA/RNA SynthesisOrthopoxvirusHepatitis B virusnucleosideanaloghalf-lifetoxicitylowpolymeraseInhibitorinhibitorinhibit