160707-69-7
160707-69-7 structure
- Name: Apricitabine
- Chemical Name: 4-amino-1-[(2R,4R)-2-(hydroxymethyl)-1,3-oxathiolan-4-yl]pyrimidin-2-one
- CAS Number: 160707-69-7
- Molecular Formula: C8H11N3O3S
- Molecular Weight: 229.256
- Catalog: Signaling Pathways Anti-infection HIV
- Create Date: 2018-05-14 08:00:00
- Modify Date: 2024-02-02 08:16:59
-
Apricitabine (SPD754; AVX754), the (-) enantiomer of 2′-deoxy-3′-oxa-4′-thiocytidine (dOTC), is a highly selective and orally active HIV-1 reverse transcriptase (RT) inhibitor (Ki=0.08 μM), as well as inhibits DNA polymerases α, β, and γ with Ki value of 300 μM, 12 μM, and 112.25 μM, respectively[1]. Apricitabine (SPD754; AVX754) shows promising antiretroviral efficacy, good tolerability and a low propensity for resistance selection in antiretroviral-naive HIV infection[2].
| Name | 4-amino-1-[(2R,4R)-2-(hydroxymethyl)-1,3-oxathiolan-4-yl]pyrimidin-2-one |
|---|---|
| Synonyms |
4-amino-1-[(2R,4R)-2-(hydroxymethyl)-1,3-oxathiolan-4-yl]pyrimidin-2(1H)-one
SPD754 AVX754 4-Amino-1-[(2R,4R)-2-(hydroxymethyl)-1,3-oxathiolan-4-yl]-2(1H)-pyrimidinone 2(1H)-Pyrimidinone, 4-amino-1-[(2R,4R)-2-(hydroxymethyl)-1,3-oxathiolan-4-yl]- Apricitabine |
| Description | Apricitabine (SPD754; AVX754), the (-) enantiomer of 2′-deoxy-3′-oxa-4′-thiocytidine (dOTC), is a highly selective and orally active HIV-1 reverse transcriptase (RT) inhibitor (Ki=0.08 μM), as well as inhibits DNA polymerases α, β, and γ with Ki value of 300 μM, 12 μM, and 112.25 μM, respectively[1]. Apricitabine (SPD754; AVX754) shows promising antiretroviral efficacy, good tolerability and a low propensity for resistance selection in antiretroviral-naive HIV infection[2]. |
|---|---|
| Related Catalog | |
| Target |
HIV-1 |
| 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 agsinst 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 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) (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]. 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]. |
| References |
| Density | 1.7±0.1 g/cm3 |
|---|---|
| Boiling Point | 475.4±55.0 °C at 760 mmHg |
| Molecular Formula | C8H11N3O3S |
| Molecular Weight | 229.256 |
| Flash Point | 241.3±31.5 °C |
| Exact Mass | 229.052109 |
| PSA | 115.67000 |
| LogP | -1.35 |
| Vapour Pressure | 0.0±2.7 mmHg at 25°C |
| Index of Refraction | 1.755 |