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Technical Data
| Formula | C14H18N6O |
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| Molecular Weight | 286.33 | CAS No. | 136470-78-5 | |
| Solubility (25°C)* | In vitro | DMSO | 57 mg/mL (199.07 mM) | |
| Ethanol | 57 mg/mL (199.07 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | Abacavir is a powerful nucleoside analog reverse transcriptase inhibitor (NRTI) used to treat HIV and AIDS. | |
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| 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 Assay:[2] |
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| Animal Study:[2] |
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References
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Selleck's Abacavir has been cited by 9 publications
| Biological and Structural Analyses of New Potent Allosteric Inhibitors of HIV-1 Integrase [ Antimicrob Agents Chemother, 2023, 67(7):e0046223] | PubMed: 37310224 |
| Reverse Transcriptase Inhibition Disrupts Repeat Element Life Cycle in Colorectal Cancer [ Cancer Discov, 2022, candisc.1117.2021] | PubMed: 35320348 |
| Defining stable reference genes in HIV latency reversal experiments [ J Virol, 2021, JVI.02305-20] | PubMed: 33762410 |
| Antiretroviral Drugs Regulate Epigenetic Modification of Cardiac Cells Through Modulation of H3K9 and H3K27 Acetylation [ Front Cardiovasc Med, 2021, 8:634774] | PubMed: 33898535 |
| Differential Interactome Based Drug Repositioning Unraveled Abacavir, Exemestane, Nortriptyline Hydrochloride, and Tolcapone as Potential Therapeutics for Colorectal Cancers [ Front Bioinform, 2021, 1:710591] | PubMed: 36303724 |
| SAMHD1 is active in cycling cells permissive to HIV-1 infection [Badia R, et al. Antiviral Res, 2017, 142:123-135] | PubMed: 28359840 |
| The thioacetate-ω(γ-lactam carboxamide) HDAC inhibitor ST7612AA1 as HIV-1 latency reactivation agent [Badia R, et al. Antiviral Res, 2015, 123:62-9] | PubMed: 26348004 |
| Nucleoside Reverse Transcriptase Inhibitors Suppress Laser-Induced Choroidal Neovascularization in Mice [ Invest Ophthalmol Vis Sci, 2015, 56(12):7122-9] | PubMed: 26529046 |
| SAMHD1 specifically affects the antiviral potency of thymidine analog HIV reverse transcriptase inhibitors [Ballana E, et al. Antimicrob Agents Chemother, 2014, 58(8):4804-13] | PubMed: 24913159 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.