Cas No.: | 1611493-60-7 |
Chemical Name: | Bictegravir |
Synonyms: | Bictegravir;8GB79LOJ07;Bictegravir [INN];Bictegravir [USAN:INN];GS 9883;Bictegravir (USAN/INN);BDBM330048;BCP25703;s5911;DB11799;SB18851 |
SMILES: | FC1C([H])=C(C([H])=C(C=1C([H])([H])N([H])C(C1C(C(=C2C(N3[C@@]([H])(C([H])([H])N2C=1[H])O[C@]1([H])C([H])([H])C([H])([H])[C@@]3([H])C1([H])[H])=O)O[H])=O)=O)F)F |
Formula: | C21H18F3N3O5 |
M.Wt: | 449.3799 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | Bictegravir is a novel, potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM. |
In Vitro: | Bictegravir (BIC) inhibits the strand transfer activity with an IC50 of 7.5± 0.3 nM. Relative to its inhibition of strand transfer activity, Bictegravir is a much weaker inhibitor of 3′-processing activity of HIV-1 IN, with an IC50 of 241±51 nM. Bictegravir enhances the accumulation of 2-LTR circles ~5-fold relative to the mock-treated control and reduces the amount of authentic integration products in infected cells by 100-fold. Bictegravir potently inhibits HIV-1 replication in both MT-2 and MT-4 cells with EC50s of 1.5 and 2.4 nM, respectively. Bictegravir exhibits potent antiviral effects in both primary CD4+ T lymphocytes and monocyte-derived macrophages, with EC50s of 1.5±0.3 nM and 6.6±4.1 nM, respectively, which are comparable to values obtained in T-cell lines[1]. |