Reagents and instruments for immunology, cell biology and molecular biology.

Rilpivirine [500287-72-9]

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Cat# HY-10574-50mg

Size : 50mg

Brand : MedChemExpress

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Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC₅₀=0.4 nM) and mutant viruses (EC₅₀=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV.

For research use only. We do not sell to patients.

Rilpivirine Chemical Structure

CAS No. : 500287-72-9

This product is a controlled substance and not for sale in your territory.

Based on 9 publication(s) in Google Scholar

Other Forms of Rilpivirine:

Rilpivirine-d₆ Get quote
(Z)-Rilpivirine-d₄ Get quote
Rilpivirine hydrochloride Get quote

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HIV HIV-1 HIV-2

Description

IC₅₀ & Target

HIV-1

In Vitro

R278474 is active against wild-type HIV-1 (EC₅₀=0.4 nM) and all single and double mutants tested (EC₅₀=0.1-2.0 nM)^[1].
R278474 (10-5000 nM; 30 d) does not observe the sign of wild-type HIV-1 breakthrough at 1 μM within 30 days^[1].
R278474 inhibits 81% of clinical isolates (about 1200 recombinant clinical isolates) at a 50% inhibitory concentration (EC₅₀) less than 1 nM, and inhibits 94% at EC₅₀ less than 10 nM^[1].
TMC278 shows subnanomolar EC₅₀s against wild-type HIV-1 group M isolates (0.07-1.01 nM) and nanomolar EC₅₀s against group O isolates (2.88-8.45 nM) in MT4 T-cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

R278474 (10-160 mg/kg; p.o. for 1 month) does not produce abnormal effects in rat, apart from liver weight increase and species-specific thyroid hypertrophy, both at the higher dose levels^[1].
R278474 (i.v.) exhibits elimination half-life ranges from 4.4 h in rat to 31 h in dog, and exposure (AUC_inf) amounts to 3.1 μg•h/mL (4 mg/kg) in rat, 8.7 μg•h/mL (1.25 mg/kg) in dog, 1.4 μg•h/mL (1.25 mg/ kg) in monkey, and 44•μg h/mL (1.25 mg/kg) in rabbit^[1].
R278474 (p.o.) exhibits half-life ranges between 2.8 h in rat and 39 h in dog, and oral bioavailability of 32% and 31% in rat and dog^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

366.42

Formula

C₂₂H₁₈N₆

CAS No.

500287-72-9

Appearance

Solid

Color

Light yellow to yellow

SMILES

CC1=CC(/C=C/C#N)=CC(C)=C1NC2=CC=NC(NC3=CC=C(C=C3)C#N)=N2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (136.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.7291 mL	13.6455 mL	27.2911 mL
5 mM	0.5458 mL	2.7291 mL	5.4582 mL
10 mM	0.2729 mL	1.3646 mL	2.7291 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (8.19 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 3 mg/mL (8.19 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 3 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 3 mg/mL (8.19 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.71%

Select Batch:

Data Sheet (272 KB) SDS (393 KB)

COA (243 KB) LCMS (268 KB)

Handling Instructions (2659 KB)

References

[1]. Janssen PAJ, et, al. In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine). J Med Chem. 2005 Mar 24;48(6):1901-9. [Content Brief]

[2]. Azijn H, et, al. TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. Antimicrob Agents Chemother. 2010 Feb;54(2):718-27. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.7291 mL	13.6455 mL	27.2911 mL	68.2277 mL
	5 mM	0.5458 mL	2.7291 mL	5.4582 mL	13.6455 mL
	10 mM	0.2729 mL	1.3646 mL	2.7291 mL	6.8228 mL
	15 mM	0.1819 mL	0.9097 mL	1.8194 mL	4.5485 mL
	20 mM	0.1365 mL	0.6823 mL	1.3646 mL	3.4114 mL
	25 mM	0.1092 mL	0.5458 mL	1.0916 mL	2.7291 mL
	30 mM	0.0910 mL	0.4549 mL	0.9097 mL	2.2743 mL
	40 mM	0.0682 mL	0.3411 mL	0.6823 mL	1.7057 mL
	50 mM	0.0546 mL	0.2729 mL	0.5458 mL	1.3646 mL
	60 mM	0.0455 mL	0.2274 mL	0.4549 mL	1.1371 mL
	80 mM	0.0341 mL	0.1706 mL	0.3411 mL	0.8528 mL
	100 mM	0.0273 mL	0.1365 mL	0.2729 mL	0.6823 mL

Rilpivirine Related Classifications

Anti-infection
HIV Reverse Transcriptase

Rilpivirine [500287-72-9]

Cat# HY-10574-50mg

Brand : MedChemExpress

Other Forms of Rilpivirine:

View All HIV Isoform Specific Products:

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Rilpivirine Related Classifications

Keywords:

You might also be interested by the following products:

Rilpivirine [500287-72-9]

Cat# HY-10574-50mg

Brand : MedChemExpress

Other Forms of Rilpivirine:

View All HIV Isoform Specific Products:

Rilpivirine Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Rilpivirine Related Classifications

Keywords:

You might also be interested by the following products: