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Bictegravir

CAT: 0013-GTR19162982-01Size: 1 gDry Ice: NoHazardous: No
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CAT#:0013-GTR19162982-01Size:1 g
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Description
Bictegravir (GS 9883) is a novel potent HIV-1 integrase (IN) that specifically targets IN strand transfer activity with IC50 of 7.5 nM; exhibits potent and selective in vitro antiretroviral activity in both T-cell lines and primary human T lymphocytes with EC50 of 1.5-2.4 nM, with minimal cytotoxicity; exhibits synergistic in vitro antiviral effects in pairwise combinations with tenofovir alafenamide, emtricitabine, or darunavir and maintains potent antiviral activity against HIV-1 variants.HIV Infection Phase 3 Clinical (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.
CAS Number
1611493-60-7
Product Name Alternative
GS 9883
Field of Research
Pharmacology & Drug Discovery
Purity
>98% (HPLC)
Solubility
DMSO: 80 mg/mL (< 1 mg/ml refers to the product slightly soluble or insoluble)
Smiles
C1CC2CC1N3C (O2) CN4C=C (C (=O) C (=C4C3=O) O) C (=O) NCC5=C (C=C (C=C5F) F) F
Molecular Formula
C21H18F3N3O5
Molecular Weight
449.39
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
(2R,5S,13aR) -8-hydroxy-7,9-dioxo-N- (2,4,6-trifluorobenzyl) -2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide

Alternative Products

CatalogName
BA1896-50Bictegravir

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