Etravirine

Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI). It is active against the wild-type HIV-1 strains LAI, SF2, and Ba-L (EC50s = 1.4-4.8 nM) but not the HIV-2 strain ROD (EC50 = 3,479 nM). Etravirine is also active against 18 HIV-1 strains carrrying NNRTI resistance-associated mutations (EC50s = <5 nM). Etravirine (5 µM) increases intracellular processing of the viral polyproteins Gag and Gag-Pol and decreases viral particle production in HEK293T cells transfected with a plasmid encoding the NL4.3 infectious molecular clone of HIV-1. Formulations containing etravirine have been used in the treatment of HIV-1 infection.Formal Name: 4-[[6-amino-5-bromo-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethyl-benzonitrile. CAS Number: 269055-15-4. Synonyms: R165335, TMC125. Molecular Formula: C20H15BrN6O. Formula Weight: 435.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:3): 0.25 mg/ml, DMSO: 20 mg/ml. lambdamax: 234, 310 nm. SMILES: CC1=CC(C#N)=CC(C)=C1OC2=NC(NC3=CC=C(C#N)C=C3)=NC(N)=C2Br. InChi Code: InChI=1S/C20H15BrN6O/c1-11-7-14(10-23)8-12(2)17(11)28-19-16(21)18(24)26-20(27-19)25-15-5-3-13(9-22)4-6-15/h3-8H,1-2H3,(H3,24,25,26,27). InChi Key: PYGWGZALEOIKDF-UHFFFAOYSA-N.