Cat. No.: HY-B0017

Telbivudine

(Synonyms: Epavudine; L-Thymidine; NV 02B)

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Telbivudine (Epavudine), an orally active thymidine nucleoside analog, is a potent antiviral inhibitor of hepatitis B virus (HBV) replication.

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Pureté: 99.92%
CAS No.: 3424-98-4
Formule: C₁₀H₁₄N₂O₅
Masse moléculaire:242.23

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Telbivudine Chemical Structure

CAS No.: 3424-98-4

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- Essai clinique
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Telbivudine (Epavudine), an orally active thymidine nucleoside analog, is a potent antiviral inhibitor of hepatitis B virus (HBV) replication^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	713.9 μM Compound: telbivudine	Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits	[PMID: 23812503]
HEK293	EC₅₀	>600 μM Compound: Telbivudine	Antiviral activity against HIV1 expressing reverse transcriptase D67N/K70R/T215F/K219E/M184V mutant infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 expressing reverse transcriptase D67N/K70R/T215F/K219E/M184V mutant infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	>600 μM Compound: Telbivudine	Antiviral activity against HIV1 expressing reverse transcriptase K103N/Y181C/G190A mutant infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 expressing reverse transcriptase K103N/Y181C/G190A mutant infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	>600 μM Compound: Telbivudine	Antiviral activity against HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	>600 μM Compound: Telbivudine	Antiviral activity against HIV1 subtype A isolate 1 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 subtype A isolate 1 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	>600 μM Compound: Telbivudine	Antiviral activity against HIV1 subtype A isolate 2 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 subtype A isolate 2 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	>600 μM Compound: Telbivudine	Antiviral activity against HIV1 subtype B isolate 3 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 subtype B isolate 3 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	>600 μM Compound: Telbivudine	Antiviral activity against HIV1 subtype B isolate 4 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 subtype B isolate 4 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	>600 μM Compound: Telbivudine	Antiviral activity against HIV1 subtype BF isolate 5 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 subtype BF isolate 5 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	>600 μM Compound: Telbivudine	Antiviral activity against HIV1 subtype C isolate 6 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 subtype C isolate 6 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	>600 μM Compound: Telbivudine	Antiviral activity against HIV1 subtype C isolate 7 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 subtype C isolate 7 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HEK293	EC₅₀	>600 μM Compound: Telbivudine	Antiviral activity against HIV1 subtype D isolate 8 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs Antiviral activity against HIV1 subtype D isolate 8 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs	[PMID: 20308377]
HepG2 2.2.15	CC₅₀	>200 μM Compound: Telbivudine	Cytotoxicity in human HepG2.215 cells assessed as reduction in cell viability after 5 days by CCK8 assay Cytotoxicity in human HepG2.215 cells assessed as reduction in cell viability after 5 days by CCK8 assay	[PMID: 28082068]

In Vitro

Telbivudine reverses B19V-induced dysregulation of BIRC3, thus, intervening in the apoptosis pathway and protecting susceptible cells from cell death^[2].

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

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 3424-98-4
Appearance Solid
Masse moléculaire 242.23
Formule C₁₀H₁₄N₂O₅
Color White to off-white
SMILES

O=C(N1)N([C@@H]2C[C@@H](O)[C@H](CO)O2)C=C(C)C1=O
Synonyms

Epavudine; L-Thymidine; NV 02B
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Chem Biol Interact

Insights into the mechanisms of telbivudine-induced myopathy associated with mitochondrial dysfunction. [Abstract]

2023 Sep 25:383:110692. PMID: 37659625

Solvant et solubilité

In Vitro:

DMSO : 50 mg/mL (206.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 33.33 mg/mL (137.60 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.1283 mL

20.6415 mL

41.2831 mL

5 mM

0.8257 mL

4.1283 mL

8.2566 mL

10 mM

0.4128 mL

2.0642 mL

4.1283 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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: ≥ 3.25 mg/mL (13.42 mM); Clear solution

This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 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.

Protocol 2

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

Solubility: ≥ 3.25 mg/mL (13.42 mM); Clear solution

This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 3.25 mg/mL (13.42 mM); Clear solution

This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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: 10 mg/mL (41.28 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 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

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Kim JW, et al. Telbivudine: a novel nucleoside analog for chronic hepatitis B. Ann Pharmacother. 2006;40(3):472-478. [Content Brief]

[2]. Zobel T, et al. Telbivudine Reduces Parvovirus B19-Induced Apoptosis in Circulating Angiogenic Cells. Viruses. 2019;11(3):227. Published 2019 Mar 6. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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 / DMSO	1 mM	4.1283 mL	20.6415 mL	41.2831 mL	103.2077 mL
	5 mM	0.8257 mL	4.1283 mL	8.2566 mL	20.6415 mL
	10 mM	0.4128 mL	2.0642 mL	4.1283 mL	10.3208 mL
	15 mM	0.2752 mL	1.3761 mL	2.7522 mL	6.8805 mL
	20 mM	0.2064 mL	1.0321 mL	2.0642 mL	5.1604 mL
	25 mM	0.1651 mL	0.8257 mL	1.6513 mL	4.1283 mL
	30 mM	0.1376 mL	0.6881 mL	1.3761 mL	3.4403 mL
	40 mM	0.1032 mL	0.5160 mL	1.0321 mL	2.5802 mL
	50 mM	0.0826 mL	0.4128 mL	0.8257 mL	2.0642 mL
	60 mM	0.0688 mL	0.3440 mL	0.6881 mL	1.7201 mL
	80 mM	0.0516 mL	0.2580 mL	0.5160 mL	1.2901 mL
	100 mM	0.0413 mL	0.2064 mL	0.4128 mL	1.0321 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.

Keywords

Telbivudine

1 Cited Publications

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Telbivudine

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Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Telbivudine

Anti-Infection Compound Library

FDA-Approved Drug Library

Antiviral Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Drug-Induced Liver Injury (DILI) Compound Library

Rare Diseases Drug Library

EMA-Approved Drug Library

Human Metabolite Library

Off-patent Drug Library

Mitochondrial Toxicity Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Telbivudine

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Telbivudine Related Classifications

HY-B0017 Related Classifications