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Apricitabine

Catalog No. T14313   CAS 160707-69-7
Synonyms: AVX754, SPD754

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.

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Apricitabine Chemical Structure
Apricitabine, CAS 160707-69-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 50.00
5 mg In stock $ 93.00
10 mg In stock $ 134.00
25 mg In stock $ 225.00
50 mg In stock $ 354.00
100 mg In stock $ 585.00
1 mL * 10 mM (in DMSO) In stock $ 95.00
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Biological Description
Chemical Properties
Storage & Solubility Information
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, HIV-1IIIB:20 μM, Lamivudine-resistant:21 μM, Zidovudine-resistant:30 μM, Wild-type (control):25 μM, Abacavir-resistant:32 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]
Synonyms AVX754, SPD754
Molecular Weight 229.26
Formula C8H11N3O3S
CAS No. 160707-69-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 11 mg/mL (47.98 mM)

TargetMolReferences and Literature

1. de Muys JM, et al. Anti-human immunodeficiency virus type 1 activity, intracellular metabolism, and pharmacokinetic evaluation of 2'-deoxy-3'-oxa-4'-thiocytidine.Antimicrob Agents Chemother. 1999 ; 43(8):1835-1844. 2. Cahn P, et al. Efficacy and tolerability of 10-day monotherapy with apricitabine in antiretroviral-naive, HIV-infected patients.AIDS. 2006 ; 20(9):1261-1268. 3. Gaffney MM, et al. Apricitabine: a nucleoside reverse transcriptase inhibitor for HIV infection. Ann Pharmacother. 2009 ; 43(10):1676-1683. 4. Cahn P, et al. Resistance profile of the new nucleoside reverse transcriptase inhibitor apricitabine. J Antimicrob Chemother. 2010 ; 65(2):213-217.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Highly Selective Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Viral Compound Library DNA Damage & Repair Compound Library Bioactive Compound Library Inhibitor Library Anti-Cancer Compound Library Bioactive Compounds Library Max Clinical Compound Library

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Keywords

Apricitabine 160707-69-7 Cell Cycle/Checkpoint DNA Damage/DNA Repair Microbiology/Virology Proteases/Proteasome DNA/RNA Synthesis HIV Protease SPD-754 AVX754 SPD 754 SPD754 AVX 754 AVX-754 inhibitor inhibit

 

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