product name Rilpivirine
Description: Rilpivirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV-1 infection. Rilpivirine is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) with higher potency, longer half-life and reduced side-effect profile compared with older NNRTIs, such as efavirenz. Rilpivirine showed inhibitory activities to both wild-type HIV (with EC50 value of 0.51 nM) and NNRTI-resistant strains. The conformational flexibility of rilpivirine allowed it to adjust different mutations of the reverse transcriptase. For the singly mutant HIV strains such as L100I, G190S, G190A and V106A, rilpivirine showed higher retained potency than efavirenz and low EC50 values blow 1 nM.
References: J Med Chem. 2005 Mar 24;48(6):1901-9; Antimicrob Agents Chemother. 2010 Feb;54(2):718-27.
366.42
Formula
C22H18N6
CAS No.
500287-72-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 73 mg/mL (199.2 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
R278474, TMC278
other peoduct :
| In Vitro |
In vitro activity: Rilpivirine shows antiviral activity with EC50 ranging from 0.1 nM to 2 nM against wild-type and selected site-directed single and double mutants of HIV-1. Rilpivirine inhibits viral replication at concentrations at which first-generation NNRTIs could not suppress replication, and produces a high genetic barrier to resistance development. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | After iv administration of Rilpivirine, Elimination half-life ranges from 4.4 h in rat to 31 h in dog. After oral administration of Rilpivirine in PEG 400, half-life ranges between 2.8 h in rat and 39 h in dog. |
| Animal model | Sprague−Dawley rat, beagle dog, white New Zealand rabbit, and cynomolgus monkey. |
| Formulation & Dosage | Dissolved in PEG 400; 4 mg/kg ( rat); 1.25 mg/kg (other species); i.v. or p.o. |
| References | J Med Chem. 2005 Mar 24;48(6):1901-9; Antimicrob Agents Chemother. 2010 Feb;54(2):718-27. |
