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Rilpivirine

Catalog No. T2330 CAS 500287-72-9

Synonyms: TMC278, R278474, DB08864

Rilpivirine (R278474) is a diarylpyrimidine derivative and reverse transcriptase inhibitor with antiviral activity against HIV-1 that is used in the treatment of HIV infections.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Rilpivirine, CAS 500287-72-9

Pack Size	Availability	Price/USD
2 mg	In stock	$ 32.00
5 mg	In stock	$ 50.00
10 mg	In stock	$ 80.00
25 mg	In stock	$ 148.00
50 mg	In stock	$ 255.00
100 mg	In stock	$ 378.00
500 mg	In stock	$ 886.00
1 mL * 10 mM (in DMSO)	In stock	$ 73.00

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Purity: 98.83%

Purity: 98.45%

Purity: 98.41%

Purity: 98%

Purity: 97.42%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Rilpivirine (R278474) is a diarylpyrimidine derivative and reverse transcriptase inhibitor with antiviral activity against HIV-1 that is used in the treatment of HIV infections.
In vitro	Rilpivirine, dissolved in PEG 400 and administered via intravenous injection at dosages of 4 mg/kg in rats and 1.25 mg/kg in dogs, exhibits half-lives of 4.4 hours and 31 hours, respectively.
In vivo	Rilpivirine demonstrates antiviral activity against both wild-type and selective point single and double HIV-1 mutants, with an effective concentration (EC50) ranging from 0.1 to 2 nM.

Synonyms	TMC278, R278474, DB08864
Molecular Weight	366.42
Formula	C22H18N6
CAS No.	500287-72-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 68 mg/mL (185.6 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Janssen PA, et al. J Med Chem. 2005, 48(6), 1901-1909. 2. Azijn H, et al. Antimicrob Agents Chemother. 2010, 54(2), 718-727. 3. Fical L. Vývoj UHPLC-MS/MS metody pro analýzu vybraných antivirotik v HILIC a RP módu[J]. 2020 4. Kang D, Pang X, Lian W, et al. Discovery of VEGFR2 inhibitors by integrating naïve Bayesian classification, molecular docking and drug screening approaches[J]. RSC Advances. 2018 Jan 8(10): 5286-5297. 5. Fical L, Khalikova M, Kočová Vlčková H, et al. Determination of Antiviral Drugs and Their Metabolites Using Micro-Solid Phase Extraction and UHPLC-MS/MS in Reversed-Phase and Hydrophilic Interaction Chromatography Modes[J]. Molecules. 2021, 26(8): 2123.

Citations

1. Bao H, Yan J, Huang J, et al.Activation of endogenous retrovirus triggers microglial immuno-inflammation and contributes to negative emotional behaviors in mice with chronic stress.Journal of Neuroinflammation.2023, 20(1): 1-16. 2. Liu K, Hao Z, Zheng H, et al.Repurposing of rilpivirine for preventing platelet β3 integrin-dependent thrombosis by targeting c-Src active autophosphorylation.Thrombosis Research.2023 3. Islam S, Rahaman M H, Yu M, et al.Anti-Leukaemic Activity of Rilpivirine Is Mediated by Aurora A Kinase Inhibition.Cancers.2023, 15(4): 1044. 4. Fical L, Khalikova M, Kočová Vlčková H, et al. Determination of Antiviral Drugs and Their Metabolites Using Micro-Solid Phase Extraction and UHPLC-MS/MS in Reversed-Phase and Hydrophilic Interaction Chromatography Modes. Molecules. 2021, 26(8): 2123. 5. Kang D, Pang X, Lian W, et al. Discovery of VEGFR2 inhibitors by integrating naïve Bayesian classification, molecular docking and drug screening approaches. RSC Advances. 2018 Jan 8(10): 5286-5297.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Inhibitor Library EMA Approved Drug Library NO PAINS Compound Library FDA-Approved Drug Library Immunology/Inflammation Compound Library Bioactive Compounds Library Max Human Metabolite Library Bioactive Compound Library FDA-Approved & Pharmacopeia Drug Library

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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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Rilpivirine 500287-72-9 Microbiology/Virology Proteases/Proteasome Reverse Transcriptase HIV Protease antiviral diarylpyrimidine DAPY transcriptase TMC-278 reverse TMC278 DB-08864 Inhibitor R278474 Human immunodeficiency virus mutant DB 08864 NNRTI wild-type non-nucleoside R 278474 inhibit R-278474 TMC 278 resistance DB08864 HIV inhibitor

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