(+-)-Efavirenz-d5

(+-)-Efavirenz-d5 is intended for use as an internal standard for the quantification of efavirenz (Item No. 14412) by GC- or LC-MS. Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that binds to wild-type and mutant HIV-1 RTs (Kis = 2.93 and 3.85-56.5 nM, respectively).{42187} It inhibits wild-type and mutant HIV-1 viral replication in MT-4 human T lymphoid cells (IC95s = 1.5-1,500 nM). Efavirenz also prevents RNA plus-strand initiation with an IC50 value of 17 nM.{22819} In vivo, efavirenz reduces HIV-1 cDNA in spleen of HIV-1-challenged HIV-susceptible transgenic rats.{42188} Formulations containing efavirenz have been used in combination therapy for the treatment of HIV-1.{22821,22820}