Apricitabine

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].

Product Specifications

CAS Number

[160707-69-7]

Product Name Alternative

SPD754; AVX754

UNSPSC

12352005

Target

DNA/RNA Synthesis; HIV; Nucleoside Antimetabolite/Analog

Type

Reference compound

Related Pathways

Anti-infection; Cell Cycle/DNA Damage

Applications

COVID-19-anti-virus

Field of Research

Infection

Assay Protocol

https://www.medchemexpress.com/apricitabine.html

Purity

99.8

Solubility

10 mM in DMSO

Smiles

O=C1N=C(N)C=CN1[C@@H]2S[C@H](CO)OC2

Molecular Formula

C8H11N3O3S

Molecular Weight

229.26

References & Citations

[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 Aug;43 (8) :1835-44.|[2]Cahn P, et al. Efficacy and tolerability of 10-day monotherapy with apricitabine in antiretroviral-naive, HIV-infected patients.AIDS. 2006 Jun 12;20 (9) :1261-8.

Shipping Conditions

Blue Ice

Storage Conditions

-20°C, 3 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 3

Isoform

HIV-1