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Apricitabine (Synonyms: SPD754, AVX754)

Catalog No. T14313 Copy Product Info
Purity: 99.45%
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Apricitabine (SPD754) is a highly selective and orally active HIV-1 reverse transcriptase inhibitor (Ki=0.08 μM), the (-) enantiomer of 2′-deoxy-3′-oxy-4′-thiocytidine (dOTC) . Apricitabine inhibits DNA polymerase α, β and γ with Ki values of 300 μM, 12 μM and 112.25 μM, respectively. Apricitabine has shown good antiretroviral therapeutic efficacy in antiretroviral HIV-infected patients, with good tolerability and low selective resistance.

Apricitabine

Copy Product Info
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Catalog No. T14313
Synonyms SPD754, AVX754

Apricitabine (SPD754) is a highly selective and orally active HIV-1 reverse transcriptase inhibitor (Ki=0.08 μM), the (-) enantiomer of 2′-deoxy-3′-oxy-4′-thiocytidine (dOTC) . Apricitabine inhibits DNA polymerase α, β and γ with Ki values of 300 μM, 12 μM and 112.25 μM, respectively. Apricitabine has shown good antiretroviral therapeutic efficacy in antiretroviral HIV-infected patients, with good tolerability and low selective resistance.

Apricitabine
Cas No. 160707-69-7
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Pack SizePriceUSA StockGlobal StockQuantity
1 mg$57In StockIn Stock
5 mg$136In StockIn Stock
10 mg$196In StockIn Stock
25 mg$339In StockIn Stock
50 mg$493In StockIn Stock
1 mL x 10 mM (in DMSO)$128In StockIn Stock
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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Purity:99.45%
ee:100%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Apricitabine (SPD754) is a highly selective and orally active HIV-1 reverse transcriptase inhibitor (Ki=0.08 μM), the (-) enantiomer of 2′-deoxy-3′-oxy-4′-thiocytidine (dOTC) . Apricitabine inhibits DNA polymerase α, β and γ with Ki values of 300 μM, 12 μM and 112.25 μM, respectively. Apricitabine has shown good antiretroviral therapeutic efficacy in antiretroviral HIV-infected patients, with good tolerability and low selective resistance.
Targets&IC50
Zidovudine-resistant:30 μM, Zidovudine-resistant/lamivudine-resistant:55 μM, Lamivudine-resistant:21 μM, Abacavir resistant:32 μM, Wild-type (control):25 μM, HIV-1 (IIIB):20 μM
In vitro
Apricitabine (SPD754 ; AVX754) is against clinical isolates of HIV-1 in cultured PBMCs with IC50 values of 0.2 μM, 1.45 μM, 2.2 μM and 2.4 μM for HIV-1RF, Wild type, 3TC resistant, 3TC and AZT resistant, respectively[1].
Apricitabine (SPD754 ; AVX754) has antiviral activities against HIV-1 clinical isolates resistant to nucleoside reverse transcriptase inhibitors in MT-4 cells, exhibits Mean IC50 values of 20 μM, 25 μM, 30 μM,21 μM,55 μM,32 μM and 71 μM. It is for HIV-1IIIB, Wild-type(control), Zidovudine-resistant/lamivudine-resistant, Zidovudine-resistant, Lamivudine-resistant, Abacavir-resistant and Stavudine-resistant viruses, respectively.[2]
In vivo
Apricitabine (SPD754 ; AVX754) (intravenous injection ; 10 mg/kg ; once a day) exhibits the T1/2, AUC0–∞ values of 12.7 mins, 226.9 μg/min/ml in female rats[1]. Apricitabine (SPD754 ; AVX754) (oral adminstation ; 10 mg/kg ; once a day) exhibits a good oral bioavailability of 68% for males and 69.4% for females rats and the T1/2, AUC0–∞, Tmax, Cmax are 62.2 mins, 157.4 μg/min/ml and 37.3 mins, 1.16 μg/ml in female rats.[1]
SynonymsSPD754, AVX754
Chemical Properties
Molecular Weight229.26
FormulaC8H11N3O3S
Cas No.160707-69-7
SmilesO=C1N([C@@H]2S[C@H](CO)OC2)C=CC(N)=N1
Relative Density.1.73
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 11 mg/mL (47.98 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM4.3619 mL21.8093 mL43.6186 mL218.0930 mL
5 mM0.8724 mL4.3619 mL8.7237 mL43.6186 mL
10 mM0.4362 mL2.1809 mL4.3619 mL21.8093 mL
20 mM0.2181 mL1.0905 mL2.1809 mL10.9046 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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