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Technical Data
| Formula | C23H23ClFNO5 |
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| Molecular Weight | 447.88 | CAS No. | 697761-98-1 | |
| Solubility (25°C)* | In vitro | DMSO | 89 mg/mL (198.71 mM) | |
| Ethanol | 35 mg/mL (78.14 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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Preparing Stock Solutions
Biological Activity
| Description | Elvitegravir is an HIV integrase inhibitor for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM in cell-free assays, respectively. | ||||||
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| In vitro | Elvitegravir inhibits PBMC and PA with IC50 of 0.89 and 20 nM, respectively. Elvitegravir prevents the integration of HIV-1 cDNA through the inhibition of DNA strand transfer. Elvitegravir suppresses the replication of HIV-1, including various subtypes and multiple-drug-resistant clinical isolates, and HIV-2 strains with a 50% effective concentration in the subnanomolar to nanomolar range. Elvitegravir inhibits the replication of HIV-1 clinical isolates carrying NRTI, NNRTI, and PI resistance-associated genotypes. Elvitegravir inhibits the HIV replication at a step that occurs after reverse transcription but before proteolytic cleavage, consistent with the integration step. Elvitegravir inhibits the synthesis of strand transfer products with an IC50 of 54 nM. Elvitegravir blocks integration via the inhibition of IN-mediated strand transfer. [1] Elvitegravir inhibits the integration of the HIV-based vector used as a positive control for the luciferase assay with an EC50 of 0.8 nM, as observed in the MAGI assay with HIV-1IIIB. Elvitegravir suppresses the replication of MLV infection with IC50 of 5.8 nM as well as that of the primate retrovirus SIV (IC50 = 0.5 nM), revealing that IN inhibitors have antiviral activity against a broad range of retroviruses. EVG is active against HIV-1 and HIV-2 and has a serum-free antiviral IC50 of 0.3-0.9 nM in peripheral blood mononuclear cells. [2] |
Protocol (from reference)
References
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Customer Product Validation
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Data from [J Antimicrob Chemother, 2011, 66, 802-812]
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Data from [J Antimicrob Chemother, 2011, 66, 802-812]
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Data from [J Antimicrob Chemother, 2011, 66, 802-812]
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Data from [Antim Ag Ch, 2011, 55, 42-49]
Selleck's Elvitegravir has been cited by 32 publications
| Biological and Structural Analyses of New Potent Allosteric Inhibitors of HIV-1 Integrase [ Antimicrob Agents Chemother, 2023, 67(7):e0046223] | PubMed: 37310224 |
| Acute antagonism in three-drug combinations for vaginal HIV prevention in humanized mice [ Sci Rep, 2023, 13(1):4594] | PubMed: 36944714 |
| Anti-HIV drug elvitegravir suppresses cancer metastasis via increased proteasomal degradation of m6A methyltransferase METTL3 [ Cancer Res, 2022, canres.4124.2021] | PubMed: 35507004 |
| In Vitro Susceptibility of HIV Isolates with High Growth Capability to Antiretroviral Drugs [ Int J Mol Sci, 2022, 23(23)15380] | PubMed: 36499705 |
| Reduction of CD8 T cell functionality but not inhibitory capacity by integrase inhibitors [ J Virol, 2022, JVI0173021] | PubMed: 35019724 |
| Impact of combinations of clinically observed HIV integrase mutations on phenotypic resistance to integrase strand transfer inhibitors (INSTIs): a molecular study [ J Antimicrob Chemother, 2022, dkab498] | PubMed: 35061879 |
| Biochemical Activity of RAGs Is Impeded by Dolutegravir, an HIV Integrase Inhibitor [ Cell Death Discov, 2020, 6:50] | PubMed: 32566255 |
| Effect of HIV infection and antiretroviral therapy on immune cellular functions. [ JCI Insight, 2019, 4(12)] | PubMed: 31217351 |
| HIV-1 Subtype C with PYxE Insertion Has Enhanced Binding of Gag-p6 to Host Cell Protein ALIX and Increased Replication Fitness. [ J Virol, 2019, 93(9)] | PubMed: 30760577 |
| Accumulation of Multiple Mutations In Vivo Confers Cross-Resistance to New and Existing Integrase Inhibitors. [ J Infect Dis, 2018, 218(11):1773-1776] | PubMed: 30010985 |
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.