Description:
Bictegravir is a novel, potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM for strand transfer activity. Bictegravir is a drug of the integrase inhibitor class that was copied from Dolutegravir by scientists at Gilead Sciences. 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). In 2016, bictegravir was in a Phase 3 trial as part of a single tablet regimen in combination with tenofovir alafenamide (TAF) and emtricitabine (FTC) for the treatment of HIV-1 infection.
- Molecular Weight: 449.39
- Molecular Formula: C21H18F3N3O5
Purity: ≥98%
Canonical SMILES:
C1CC2CC1N3C(O2)CN4C=C(C(=O)C(=C4C3=O)O)C(=O)NCC5=C(C=C(C=C5F)F)F
InChI:
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
InChIKey: SOLUWJRYJLAZCX-LYOVBCGYSA-N
- Boiling Point: 682.5±55.0 °C at 760 mmHg
- Solubility: Soluble in DMSO.
- Appearance: Off-white to yellow powder
- Storage: 2-8°C
Synonyms:
GS-9883; GS 9883; GS9883
More details are to be found on supplier website
