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Apricitabine

🥰Excellent
Catalog No. T14313Cas No. 160707-69-7
Alias 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

Apricitabine

🥰Excellent
Purity: 100%
Catalog No. T14313Alias SPD754, AVX754Cas No. 160707-69-7
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.
Pack SizePriceAvailabilityQuantity
1 mg$314In Stock
5 mg$564In Stock
10 mg$698In Stock
25 mg$1,068In Stock
50 mg$1,779In Stock
100 mg$2,980In Stock
1 mL x 10 mM (in DMSO)$657In Stock
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Purity:100%
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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/lamivudine-resistant:55 μM, Zidovudine-resistant:30 μM, Abacavir resistant:32 μM, Wild-type (control):25 μM, Lamivudine-resistant:21 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]
AliasSPD754, 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.
Solubility Information
DMSO: 11 mg/mL (47.98 mM)
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

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