Bictegravir

Bictegravir is an inhibitor of HIV-1 integrase (IC50 = 7.5 nM for strand transfer activity). It has antiviral activity against clinical isolates of HIV-1 in human peripheral blood mononuclear cells (PBMCs, EC50s = 0.04-1.7 nM). Bictegravir also inhibits HIV-1 viral infection in MT-2 and MT-4 cells, CD4+ T cells, and macrophages (EC50s = 1.5, 2.5, 1.5, and 6.6 nM, respectively) without exhibiting cytotoxicity (CC50s = 10.3, 3.7, 13, and 29.8 µM, respectively). Formulations containing bictegravir in combination with emtricitabine and tenofovir alafenamide have been used in the treatment of HIV-1 infections.Formal Name: (2R,5S,13aR)-2,3,4,5,7,9,13,13a-octahydro-8-hydroxy-7,9-dioxo-N-[(2,4,6-trifluorophenyl)methyl]-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide. CAS Number: 1611493-60-7. Synonyms: GS-9883. Molecular Formula: C21H18F3N3O5. Formula Weight: 449.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: soluble, Methanol: soluble. lambdamax: 248, 260, 322 nm. SMILES: FC1=CC(F)=C(CNC(C2=CN(C[C@](O[C@@]3([H])C[C@]4([H])CC3)([H])N4C5=O)C5=C(O)C2=O)=O)C(F)=C1. InChi Code: InChI=1S/C21H18F3N3O5/c22-9-3-14(23)12(15(24)4-9)6-25-20(30)13-7-26-8-16-27(10-1-2-11(5-10)32-16)21(31)17(26)19(29)18(13)28/h3-4,7,10-11,16,29H,1-2,5-6,8H2,(H,25,30)/t10-,11+,16+/m0/s1. InChi Key: SOLUWJRYJLAZCX-LYOVBCGYSA-N.