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Technical Data
| Formula | C22H18N6 |
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| Molecular Weight | 366.42 | CAS No. | 500287-72-9 | |
| Solubility (25°C)* | In vitro | DMSO | 73 mg/mL (199.22 mM) | |
| Water | Insoluble | |||
| Ethanol | 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 | Rilpivirine (R278474, TMC27, DB08864) is a non-nucleoside reverse transcriptase inhibitor (NNRTI), and used to treat HIV-1 infection. | |
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| In vitro | Rilpivirine shows antiviral activity with EC50 ranging from 0.1 nM to 2 nM against wild-type and selected site-directed single and double mutants of HIV-1. [1] Rilpivirine inhibits viral replication at concentrations at which first-generation NNRTIs could not suppress replication, and produces a high genetic barrier to resistance development. [2] | |
| In vivo | After iv administration of Rilpivirine, Elimination half-life ranges from 4.4 h in rat to 31 h in dog. After oral administration of Rilpivirine in PEG 400, half-life ranges between 2.8 h in rat and 39 h in dog. [1] | |
| Features | Approved anti-HIV drug with longer half-life and reduced side-effect profile than older NNRTIs. |
Protocol (from reference)
| Animal Study:[1] |
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References
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Selleck's Rilpivirine has been cited by 15 publications
| Chemical inhibition of DPP9 sensitizes the CARD8 inflammasome in HIV-1-infected cells [ Nat Chem Biol, 2023, 19(4):431-439] | PubMed: 36357533 |
| Biological and Structural Analyses of New Potent Allosteric Inhibitors of HIV-1 Integrase [ Antimicrob Agents Chemother, 2023, 67(7):e0046223] | PubMed: 37310224 |
| Reduction of CD8 T cell functionality but not inhibitory capacity by integrase inhibitors [ J Virol, 2022, JVI0173021] | PubMed: 35019724 |
| Biodegradable polymeric solid implants for ultra-long-acting delivery of single or multiple antiretroviral drugs [ Int J Pharm, 2021, 605:120844] | PubMed: 34216767 |
| High levels of LINE-1 transposable elements expressed in Kaposi's sarcoma-associated herpesvirus-related primary effusion lymphoma [ Oncogene, 2020, 10.1038/s41388-020-01549-9] | PubMed: 33188297 |
| Altered Gut Microbiome under Antiretroviral Therapy: Impact of Efavirenz and Zidovudine [ ACS Infect Dis, 2020, 10.1021/acsinfecdis.0c00536] | PubMed: 33346662 |
| Effect of HIV infection and antiretroviral therapy on immune cellular functions. [ JCI Insight, 2019, 4(12)] | PubMed: 31217351 |
| Conformational Changes in HIV-1 Reverse Transcriptase that Facilitate Its Maturation. [ Structure, 2019, 27(10):1581-1593] | PubMed: 31471129 |
| 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 |
| Nonnucleoside Reverse Transcriptase Inhibitor Hypersusceptibility and Resistance by Mutation of Residue 181 in HIV-1 Reverse Transcriptase. [ Antimicrob Agents Chemother, 2019, 63(8)] | PubMed: 31160281 |
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.