2. Anti-infection Metabolic Enzyme/Protease
  3. SARS-CoV MMP
  4. Rilpivirine hydrochloride

Rilpivirine hydrochloride  (Synonyms: TMC-278 hydrochloride; TMC278 hydrochloride; TMC 278 hydrochloride)

Cat. No.: HY-10574A Purity: 99.81%
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Rilpivirine (R278474) hydrochloride is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine hydrochloride has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine hydrochloride has a high genetic barrier to resistance development of HIV.

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

Rilpivirine hydrochloride Chemical Structure

Rilpivirine hydrochloride Chemical Structure

CAS No. : 700361-47-3

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Based on 9 publication(s) in Google Scholar

Other Forms of Rilpivirine hydrochloride:

Rilpivirine hydrochloride Related Antibodies

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Description

Rilpivirine (R278474) hydrochloride is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine hydrochloride has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine hydrochloride has a high genetic barrier to resistance development of HIV[1][2].

IC50 & Target

IC50: 20±10 μM (MMP)[1] Ki: 1.5±0.27 nM (MMPs)[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)[2].

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

Rilpivirine hydrochloride Related Antibodies
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].

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

402.88

Formula

C22H19ClN6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N#CC1=CC=C(NC2=NC=CC(NC3=C(C)C=C(/C=C/C#N)C=C3C)=N2)C=C1.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (310.27 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 2.4821 mL 12.4106 mL 24.8213 mL
5 mM 0.4964 mL 2.4821 mL 4.9643 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
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C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4821 mL 12.4106 mL 24.8213 mL 62.0532 mL
5 mM 0.4964 mL 2.4821 mL 4.9643 mL 12.4106 mL
10 mM 0.2482 mL 1.2411 mL 2.4821 mL 6.2053 mL
15 mM 0.1655 mL 0.8274 mL 1.6548 mL 4.1369 mL
20 mM 0.1241 mL 0.6205 mL 1.2411 mL 3.1027 mL
25 mM 0.0993 mL 0.4964 mL 0.9929 mL 2.4821 mL
30 mM 0.0827 mL 0.4137 mL 0.8274 mL 2.0684 mL
40 mM 0.0621 mL 0.3103 mL 0.6205 mL 1.5513 mL
50 mM 0.0496 mL 0.2482 mL 0.4964 mL 1.2411 mL
60 mM 0.0414 mL 0.2068 mL 0.4137 mL 1.0342 mL
80 mM 0.0310 mL 0.1551 mL 0.3103 mL 0.7757 mL
100 mM 0.0248 mL 0.1241 mL 0.2482 mL 0.6205 mL
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Rilpivirine hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rilpivirine700361-47-3TMC-278TMC278TMC 278SARS-CoVMMPSARS coronavirusMatrix metalloproteinasesdiarylpyrimidineDAPYnon-nucleosidereversetranscriptaseNNRTIantiviralwild-typeHIVmutantresistanceInhibitorinhibitorinhibit

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