Rilpivirine HCl

SKU: orb1704098

Description

Rilpivirine hydrochloride is a potent and selective non-nucleoside reverse transcriptase inhibitor (NNRTI) used in HIV research. It exhibits antiviral activity by inhibiting HIV-1 reverse transcriptase and is applied in both in vitro antiviral assays and in vivo studies of combination antiretroviral therapies.

Research Area

Infectious Disease & Virology, Protein Biochemistry

Images & Validation

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Key Properties

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CAS Number	700361-47-3
MW	402.88
Purity	99.48% (May vary between batches)
Formula	C₂₂H₁₉ClN₆
SMILES	N(C1=C(C)C=C(/C=C/C#N)C=C1C)C2=NC(NC3=CC=C(C#N)C=C3)=NC=C2.Cl
Target	MMP,SARS-CoV
Solubility	DMSO:100 mg/mL (248.21 mM)

Bioactivity

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Target IC50	HIV-1 (wild-type):EC50=0.4 nM
In Vivo	Oral administration of Rilpivirine HCl in rats (10-160 mg/kg for 1 month) did not elicit significant abnormal responses, except for increased liver weight and species-specific thyroid hypertrophy observed at some of the higher doses. The elimination half-life of intravenously administered Rilpivirine HCl ranged from 4.4 hours in rats to 31 hours in dogs, with drug exposures (AUCinf) ranging from 3.1 μg-h/mL in rats (4 mg/kg), to 8.7 μg-h/mL in dogs (1.25 mg/kg), 1.4 μg-h/mL in monkeys (1.25 mg/kg), and 1.4 μg-h/mL in rabbits ( 1.25 mg/kg) and 44 μg-h/mL in rabbit (1.25 mg/kg). When administered orally, the half-life of Rilpivirine HCl was 2.8 hours in rats and 39 hours in dogs, with oral bioavailability of 32% and 31% in rats and dogs, respectively. Read more...
In Vitro	Rilpivirine HCl showed significant activity against wild-type HIV-1 (EC50=0.4 nM) and activity ranged from EC50=0.1-2.0 nM against all single and double mutants tested. no indication of breakthrough of wild-type HIV-1 at 1 μM was observed with Rilpivirine HCl in 30-day experiments at concentrations ranging from 10 to 5000 nM. Rilpivirine HCl was able to inhibit 81% of clinical isolates (approximately 1,200 recombinant clinical isolates) with an EC50 of less than 1 nM and 94% of clinical isolates with an EC50 of less than 10 nM. Rilpivirine HCl showed sub-nanomolar activity against HIV-1 Group M wild-type isolates with EC50s ranging from 0.07 to 1.01 nM. Read more...

Storage & Handling

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Storage	store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Rilpivirine, Rilpivirine HCl, Rilpivirine hydrochloride, SARS-CoV, SARSCoV, TMC-278 hydrochloride, TMC278 hydrochloride, TMC278, TMC-278, TMC 278. trade name Edurant, TMC 278, MMP, AQUIPTA

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Compound Identifiers

PubChem CID

11711114 ↗

Key Properties

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No computed properties available.

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Rilpivirine HCl

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Quality Guarantee

Compound Identifiers

Key Properties

Documents Download

Request a Document

Protocol Information

Rilpivirine HCl (orb1704098)

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