Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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 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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 11 mg/mL (47.98 mM)
You can also refer to dose conversion for different animals. More
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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.
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