Home Microbiology Reverse Transcriptase inhibitor Abacavir

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Abacavir Reverse Transcriptase inhibitor

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

Abacavir Reverse Transcriptase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 286.33

Purity & Quality Control

Related Products

Signaling Pathway

Reverse Transcriptase Signaling Pathways

Reverse Transcriptase Signaling Pathway

Mechanism of Action

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]. This compound induces chromosomal DSBs and thereby kills ATL cells but not non-HTLV-1-infected cells. Once it 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. This chemical 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, this compound is rapidly absorbed after oral administration, with peak concentrations occurring 0.63-1 hour after dosing. The absolute bioavailability of abacavir is approximately 83%. Its pharmacokinetics are linear and doseproportional over the range of 300-1200 mg/day. The apparent volume of distribution after intravenous administration is approximately 0.86 ± 0.15 L/kg, suggesting that it is distributed to extravascular spaces. Binding to plasma proteins is about 50% and is independent of the plasma abacavir concentration. This chemical is extensively metabolized by the liver; less than 2% is excreted as unchanged drug in the urine. It 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 is approximately 1.5 hours. The antiviral effect is due to its intracellular anabolite, carbovirtriphosphate (CBV-TP). This compound 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 --

References
  • https://pubmed.ncbi.nlm.nih.gov/16305515/
  • https://pubmed.ncbi.nlm.nih.gov/26601161/
  • https://pubmed.ncbi.nlm.nih.gov/18479171/

Chemical Information

Molecular Weight 286.33 Formula

C14H18N6O
CAS No. 136470-78-5 SDF --
Synonyms 1592U89
Smiles C1CC1NC2=C3C(=NC(=N2)N)N(C=N3)C4CC(C=C4)CO

Storage and Stability

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


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

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Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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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.

Handling Instructions

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