Bictegravir

  Cat. No.:  DC10890   Featured
Chemical Structure
1611493-60-7
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Field of application
Bictegravir is a novel, potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.
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].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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