Rilpivirine HCl

Research use only, not for human use.

Rilpivirine HCl (Rilpivirine hydrochloride) is a selective and potent non-nucleoside reverse transcriptase inhibitor (NNRTI) with antiviral activity that inhibits the HIV virus and can be used in the study of HIV infections.

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.

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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.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.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.

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Metabolic Enzyme/Protease

MMP

MMP | SARS-CoV

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700361-47-3

402.88

C22H19ClN6

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (310.27 mM; Ultrasonic )

N(C1=C(C)C=C(/C=C/C#N)C=C1C)C2=NC(NC3=CC=C(C#N)C=C3)=NC=C2.Cl

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(-20℃)

With Ice Pack

≥ 2 years