1. Anti-infection
  2. HIV
    Reverse Transcriptase
  3. Rilpivirine

Rilpivirine (Synonyms: R278474; TMC278; DB08864)

Cat. No.: HY-10574 Purity: 98.61%
Handling Instructions

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

Rilpivirine Chemical Structure

CAS No. : 500287-72-9

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Solution
10 mM * 1 mL in DMSO USD 207 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 207 In-stock
Estimated Time of Arrival: December 31
Solid
10 mg USD 188 In-stock
Estimated Time of Arrival: December 31
50 mg USD 473 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

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Description

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[1][2].

IC50 & Target

reverse transcriptase[1]
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].

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 (AUCinf) 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].

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.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (136.46 mM; Need ultrasonic)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 3 mg/mL (8.19 mM); Clear solution

*All of the co-solvents are available by MCE.
References

Purity: 98.61%

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Rilpivirine
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