Abacavir (sulfate)

Abacavir is a nucleoside analog and an inhibitor of HIV-1 reverse transcriptase (Ki = 2.1 µM for the wild-type enzyme).1 It inhibits replication of a variety of HIV-1 and HIV-2 strains, including strains resistant to 3'-azido-3'-deoxythymidine (zidovudine; Item No. 15492) or 2',3'-dideoxyinosine (didanosine; Item No. 23715), in HeLa cells stably expressing CD4 (IC50s = 5.8-21 µM). Abacavir inhibits replication of eight HIV-1 clinical isolates in phytohemagglutinin-stimulated isolated human peripheral blood lymphocytes with a mean IC50 value of 0.26 µM. It inhibits hepatitis B virus (HBV) DNA synthesis in HepG2 cells (IC50 = 7 µM) and is also active against human cytomegalovirus (CMV) strain AD169 and the Petaluma strain of feline immunodeficiency virus (FIV) in plaque reduction assays (IC50s = 32 and 0.4 µM, respectively). Formulations containing abacavir have been used in the treatment of HIV infection.WARNING This product is not for human or veterinary use.

An antiviral nucleoside analog

384.4

≥98%

Biochemicals/Antivirals/Nucleoside Reverse Transcriptase Inhibitors (NRTIs)/Nucleotides/Nucleosides/Small Molecule Inhibitors/Reverse Transcriptases

Formal_Name:(1S,4R)-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-methanol, monosulfate;Synonyms:1592U89

NC1=NC(N([C@H]2C=C[C@@H](CO)C2)C=N3)=C3C(NC4CC4)=N1.O=S(O)(O)=O

C14H18N6O • H2SO4

216699-07-9

≥ 4 years

DMSO: 0.15 mg/ml PBS (pH 7.2): 1 mg/ml

1.Choo, H.,Chong, Y. and Chu, C.K. The role of 2',3'-unsaturation on the antiviral activity of anti-HIV nucleosides against 3TC-resistant mutant (M184V). Bioorganic & Medicinal Chemistry Letters 13(12), 1993-1996 (2003).
2.Saag, M.S. Initiation of antiretroviral therapy: Implications of recent findings. Top.HIV Med. 12(3), 83-88 (2004).
3.Phillips, E.J. and Mallal, S.A. Pharmacogenetics of drug hypersensitivity. Pharmacogenomics 11(7), 973-987 (2010).