research use only

Rilpivirine Reverse Transcriptase inhibitor

Name: Rilpivirine
Brand: Selleck Chemicals
SKU: S7303
Availability: InStock
Rating: 5 (15 reviews)

Cat.No.S7303

Rilpivirine (R278474, TMC27, DB08864) is a non-nucleoside reverse transcriptase inhibitor (NNRTI), and used to treat HIV-1 infection.

Chemical Structure

Molecular Weight: 366.42

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	Bacterial Antibiotics Anti-infection Fungal Antiviral COVID-19 Parasite HIV HCV Protease SARS-CoV HIV Protease Influenza Virus β-lactamase Integrase HBV CMV Neuraminidase HCV HSV RSV Enterovirus Thioredoxin Reductase 3C-Like Protease Ribosomal Peptidyl Transferase HPV
Related Products	Dapivirine (TMC120) Salicylanilide Fangchinoline Bifendate 3'-Fluoro-3'-deoxythymidine (Alovudine) Ulonivirine Lersivirine (UK-453061) 4-Chloro-2-(trifluoroacetyl)aniline hydrochloride

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description
MT4 cells	Function assay		Antiviral activity against wild type HIV1 LAI infected in MT4 cells by EGFP based replication assay, EC50=0.001 μM
MT4 cells	Cytotoxicity assay	3 days	Cytotoxicity against human MT4 cells after 3 days by EGFP based replication assay, CC50=2 μM
human PBMC cells	Function assay		Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG001 infected in human PBMC cells by cell based assay, EC50=0.00026 μM
human TZM-bl cells	Cytotoxicity assay	4 days	Cytotoxicity against human TZM-bl cells after 4 days by XTT assay, CC50=19.4 μM
human MT4 cells	Function assay	72 h	Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay, EC50=0.0037 μM
MT2 cells	Cytotoxicity assay		Cytotoxicity in human MT2 cells assessed as inhibition of cell growth, CC50=8 μM
MT2 cells	Function assay		Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase K103N and Y181C double mutant infected in human MT2 cells assessed as inhibition of viral infection, EC50=0.002 μM
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	366.42	Formula	C₂₂H₁₈N₆	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	500287-72-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	R278474, TMC278, DB08864			Smiles	CC1=CC(=CC(=C1NC2=NC(=NC=C2)NC3=CC=C(C=C3)C#N)C)C=CC#N

Solubility

In vitro
Batch:

DMSO : 73 mg/mL (199.22 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
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.
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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.650mg/ml (9.96mM)	Taking the 1 mL working solution as an example, add 50 μL of 73 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.456mg/ml (1.24mM)	Taking the 1 mL working solution as an example, add 50 μL of 9.12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Features	Approved anti-HIV drug with longer half-life and reduced side-effect profile than older NNRTIs.
Targets/IC₅₀/Ki	Reverse transcriptase ^[1]
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] 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. ^[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 this compound in PEG 400, half-life ranges between 2.8 h in rat and 39 h in dog. ^[1]
References	[1] https://pubmed.ncbi.nlm.nih.gov/15771434/ [2] https://pubmed.ncbi.nlm.nih.gov/19933797/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06104306	Recruiting	HIV-1-infection	Gilead Sciences	December 13 2023	Phase 4
NCT05601128	Active not recruiting	HIV-1-infection\|HIV Infections\|HIV I Infection	Allegheny Singer Research Institute (also known as Allegheny Health Network Research Institute)	January 1 2023	Phase 3
NCT05112939	Active not recruiting	Healthy	Janssen Research & Development LLC	November 16 2021	Phase 1
NCT05358756	Completed	Healthy Subject	Aptorum International Limited	October 9 2021	Phase 1

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):