Home Microbiology Reverse Transcriptase inhibitor Abacavir For research use only.

Abacavir

Synonyms: 1592U89

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

Abacavir Chemical Structure

Abacavir Chemical Structure

CAS No. 136470-78-5

Purity & Quality Control

Abacavir Related Products

Signaling Pathway

Reverse Transcriptase Signaling Pathways

Reverse Transcriptase Signaling Pathway

Biological Activity

Description Abacavir is a powerful nucleoside analog reverse transcriptase inhibitor (NRTI) used to treat HIV and AIDS.
Targets
Reverse transcriptase [1]
In vitro
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models NOD/SCID mice
Dosages 75 mg/kg
Administration oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04133012 Completed
HIV-1 Infection
ANRS Emerging Infectious Diseases|ViiV Healthcare
 February 10 2020 Not Applicable
NCT02708342 Completed
HIV
IRCCS San Raffaele|Merck Sharp & Dohme LLC
 April 2016 --

Chemical Information & Solubility

Molecular Weight 286.33 Formula

C14H18N6O
CAS No. 136470-78-5 SDF --
Smiles C1CC1NC2=C3C(=NC(=N2)N)N(C=N3)C4CC(C=C4)CO
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 57 mg/mL ( (199.07 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 57 mg/mL

Water : Insoluble


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In vivo
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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.

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