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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $31 | In Stock | |
5 mg | $46 | In Stock | |
10 mg | $64 | In Stock | |
25 mg | $98 | In Stock | |
50 mg | $148 | In Stock | |
100 mg | $217 | In Stock | |
200 mg | $319 | In Stock | |
500 mg | $539 | In Stock |
Description | 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. |
Targets&IC50 | HIV-1 (wild-type):EC50=0.4 nM |
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. [1] Rilpivirine HCl showed sub-nanomolar activity against HIV-1 Group M wild-type isolates with EC50s ranging from 0.07 to 1.01 nM. [2] |
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. [1] |
Alias | TMC-278 hydrochloride, TMC278 hydrochloride, TMC 278. trade name Edurant, Rilpivirine hydrochloride, AQUIPTA |
Molecular Weight | 402.88 |
Formula | C22H19ClN6 |
Cas No. | 700361-47-3 |
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 |
Relative Density. | no data available |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (248.21 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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