Abacavir (1592U89)

Catalog No.S5215

For research use only.

Abacavir (1592U89, ABC) is a powerful nucleoside analog reverse transcriptase inhibitor (NRTI) used to treat HIV and AIDS.

Abacavir (1592U89) Chemical Structure

CAS No. 136470-78-5

Selleck's Abacavir (1592U89) has been cited by 7 Publications

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Biological Activity

Description Abacavir (1592U89, ABC) is a powerful nucleoside analog reverse transcriptase inhibitor (NRTI) used to treat HIV and AIDS.
Targets
Reverse transcriptase [1]
In vitro

Abacavir (ABC) exhibits potent in vitro antiviral activity against wild-type HIV-1 (IC50 4.0 μM, MT-4 cells)[1]. Abacavir induces chromosomal DSBs and thereby kills ATL cells but not non-HTLV-1-infected cells. Once abacavir is incorporated into the cells, it is phosphorylated in a unique stepwise anabolism to be converted to the triphosphated guanine analog carbovir (CBV) and then incorporated into host chromosomal DNA by replicative DNA polymerases, leading to premature termination of DNA replication, collapse of the replication fork, and DSB formation. Abacavir induces S/G2-phase arrest and apoptosis in ED-40515(−) cells, but not in Jurkat cells[2].

In vivo Abacavir efficiently inhibits the growth of ATL cell xenografts in NOD/SCID mice[2]. In adults, Abacavir is rapidly absorbed after oral administration, with peak concentrations occurring 0.63-1 hour after dosing. The absolute bioavailability of abacavir is approximately 83%. Abacavir pharmacokinetics are linear and doseproportional over the range of 300-1200 mg/day. The apparent volume of distribution of abacavir after intravenous administration is approximately 0.86 ± 0.15 L/kg, suggesting that abacavir is distributed to extravascular spaces. Binding to plasma proteins is about 50% and is independent of the plasma abacavir concentration. Abacavir is extensively metabolized by the liver; less than 2% is excreted as unchanged drug in the urine. Abacavir is primarily metabolized via two pathways, uridine diphosphate glucuronyltransferase and alcohol dehydrogenase, resulting in the inactive glucuronide metabolite and the inactive carboxylate metabolite. The terminal elimination half-life of abacavir is approximately 1.5 hours. The antiviral effect of abacavir is due to its intracellular anabolite, carbovirtriphosphate (CBV-TP). Abacavir is not significantly metabolized by cytochrome P450 (CYP) enzymes, nor does it inhibit these enzymes[3].

Protocol (from reference)

Cell Research:[2]
  • Cell lines: Jurkat cells
  • Concentrations: 300 μM
  • Incubation Time: 48 h
  • Method: Jurkat cells transfected with control siRNA or siTDP1 are treated with or without 300 μM ABC for 48 hours. MTS assay is conducted.
Animal Research:[2]
  • Animal Models: NOD/SCID mice
  • Dosages: 75 mg/kg
  • Administration: oral

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 286.33
Formula

C14H18N6O

CAS No. 136470-78-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC1NC2=C3C(=NC(=N2)N)N(C=N3)C4CC(C=C4)CO

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04133012 Recruiting Other: Samplings HIV-1 Infection ANRS Emerging Infectious Diseases|ViiV Healthcare February 10 2020 Not Applicable
NCT02708342 Completed -- HIV Ospedale San Raffaele|Merck Sharp & Dohme LLC April 2016 --

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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