Rilpivirine

Rilpivirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that inhibits growth of wild-type HIV with an EC50 value of 0.51nM. It is active against NNRTI-resistant HIV strains with EC50 values less than 1nM for L100I, K103N, V106A, G190A and G190S mutants in vitro. Rilpivirine also reduces growth of greater than 80% of 1,500 NNRTI-resistant clinical isolates (EC50s = <10nM), including strains containing up to eight resistance mutations. NNRTIs work by binding to and blocking HIV reverse transcriptase, which prevents HIV from replicating and lowers the amount of HIV in the blood. Rilpivirine is an antiviral anti-HIV drug, active against wild-type and NNRTI-resistant HIV-1 with higher potency, longer half-life and reduced side-effect profile compared with Efavirenz (Prod. No. AG-CR1-3751). CARD8 inflammasome senses HIV-1 protease activity. In HIV1-infected cells, CARD8 cannot detect the virus because the viral protease remains inactive as a subunit of unprocessed Gag-Pol polyprotein. HIV-1-specific non-nucleoside reverse transcriptase inhibitors (NNRTIs), such us Rilpivirine, can trigger CARD8 sensing because they bind to HIV-1 Pol and enhance intracellular Gag-Pol polyprotein dimerization, which causes premature viral protease activation. Treating HIV-1-infected macrophages and CD4+ T cells with NNRTIs leads to CARD8-mediated caspase-1 activation and pyroptotic cell death. Induction of the CARD8 inflammasome activation has led to rapid clearance of latent HIV-1 in patient CD4+ T cells after virus reactivation. Appearance: White to off-white solid. Solubility: Soluble in DMSO (5mg/ml). Warming and sonication may be needed. InChi Key: YIBOMRUWOWDFLG-ONEGZZNKSA-N Smiles: CC1=CC(/C=C/C#N)=CC(C)=C1NC2=NC(NC3=CC=C(C=C3)C#N)=NC=C2