Apricitabine

SKU: orb1707644

Description

Apricitabine (SPD754) is the (-)-enantiomer of dOTC, a potent and selective oral HIV-1 reverse transcriptase inhibitor. It demonstrates significant antiviral activity in clinical studies with a favorable resistance profile and good tolerability in patients, while showing lower affinity for host DNA polymerases.

Research Area

Cell Biology, Infectious Disease & Virology, Molecular Biology, Protein Biochemistry

Key Properties

• CAS Number: 160707-69-7
• MW: 229.26
• Purity: 99.45%
• Formula: C₈H₁₁N₃O₃S
• SMILES: O=C1N([C@@H]2S[C@H](CO)OC2)C=CC(N)=N1
• Target: Nucleoside Antimetabolite/Analog,DNA/RNA Synthesis,HIV Protease
• Solubility: DMSO:11 mg/mL (47.98 mM)

Bioactivity

• Target IC50:
  HIV-1 (IIIB):20 μM|Abacavir resistant:32 μM|Wild-type (control):25 μM|Lamivudine-resistant:21 μM|Zidovudine-resistant/lamivudine-resistant:55 μM|Zidovudine-resistant:30 μM
• 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. 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.
• 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. 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HIV-1 reverse transcriptase, HIVProtease, HIV-1, HIV Protease, AVX 754, AVX754, AVX-754, Apricitabine, DNA Synthesis, DNA polymerase α, DNA polymerase γ, DNA polymerase beta, DNASynthesis, SPD 754, SPD754, SPD-754, RNA Synthesis, RNASynthesis

Compound Identifiers

PubChem CID

455041