Rilpivirine

Catalog No.S7303 Batch:S730301

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Technical Data

Formula

C22H18N6
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
In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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.)

Preparing Stock Solutions

Biological Activity

Description Rilpivirine (R278474, TMC27, DB08864) is a non-nucleoside Reverse Transcriptase inhibitor (NNRTI), and used to treat HIV-1 infection.
Targets
Reverse transcriptase
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. This compound inhibits viral replication at concentrations at which first-generation NNRTIs could not suppress replication, and produces a high genetic barrier to resistance development.
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 this compound in PEG 400, half-life ranges between 2.8 h in rat and 39 h in dog.
Features Approved anti-HIV drug with longer half-life and reduced side-effect profile than older NNRTIs.

Protocol (from reference)

Animal Study:[1]
  • Animal Models

    Sprague−Dawley rat, beagle dog, white New Zealand rabbit, and cynomolgus monkey.

  • Dosages

    4 mg/kg ( rat); 1.25 mg/kg (other species)

  • Administration

    i.v., p.o.

References

  • https://pubmed.ncbi.nlm.nih.gov/15771434/
  • https://pubmed.ncbi.nlm.nih.gov/19933797/

Sellecks 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.