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Abacavir Reverse Transcriptase inhibitor

Cat.No.S5215

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

Batch: Purity: 99.98%
99.98

Solubility

In vitro
Batch:

DMSO : 57 mg/mL (199.07 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 57 mg/mL

Water : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 286.33 Formula

C14H18N6O

Storage (From the date of receipt)
CAS No. 136470-78-5 -- Storage of Stock Solutions

Synonyms 1592U89 SMILES C1CC1NC2=C3C(=NC(=N2)N)N(C=N3)C4CC(C=C4)CO

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
Reverse transcriptase
In vitro
Abacavir (ABC) exhibits potent in vitro antiviral activity against wild-type HIV-1 (IC50 4.0 μM, MT-4 cells). 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.
In vivo
Abacavir efficiently inhibits the growth of ATL cell xenografts in NOD/SCID mice. 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.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-08-28)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07792096 NOT_YET_RECRUITING
HIV Infection
University College, London
2026-11 PHASE3
NCT06428045 RECRUITING
High Grade Glioma
University of Miami
2025-04-15 PHASE1
NCT06356740 NOT_YET_RECRUITING
Systemic Lupus Erythematosus
Hospices Civils de Lyon
2024-09-01 PHASE2
NCT05193994 TERMINATED
Amyotrophic Lateral Sclerosis
Macquarie University, Australia
2022-02-24 PHASE3
NCT06658977 TERMINATED
Amyotrophic Lateral Sclerosis; ALS
Macquarie University, Australia
2024-11-15 PHASE3
NCT04731103 COMPLETED
Aicardi-Goutières Syndrome
University of Edinburgh
2022-08-24 PHASE2

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