1. Anti-infection
    Metabolic Enzyme/Protease
  2. HIV
    HIV Integrase

Bictegravir (Synonyms: GS-9883)

Cat. No.: HY-17605 Purity: 98.27%
Handling Instructions

Bictegravir is a novel, potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.

For research use only. We do not sell to patients.

Bictegravir Chemical Structure

Bictegravir Chemical Structure

CAS No. : 1611493-60-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 534 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 540 In-stock
Estimated Time of Arrival: December 31
10 mg USD 780 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2340 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3540 In-stock
Estimated Time of Arrival: December 31
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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Bictegravir is a novel, potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.

IC50 & Target

IC50: 7.5 nM (HIV-1 integrase)[1]

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].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : 83.3 mg/mL (185.37 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2253 mL 11.1264 mL 22.2529 mL
5 mM 0.4451 mL 2.2253 mL 4.4506 mL
10 mM 0.2225 mL 1.1126 mL 2.2253 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

MT-2 cells are infected in bulk culture with HIV-1 IIIb at a cell density of 2×106 cells/mL for 3 h at 37°C. Infected MT-2 cells receive either DMSO (mock-treated control) or Bictegravir (BIC) at a final concentration greater than or equal to 20 times their respective antiviral 50% effective concentration (EC50). These plates are incubated at 37°C for either 12 h (for late reverse transcription product quantification) or 24 h (for 2-LTR circle and Alu-LTR product quantification), after which time the cells are harvested for total DNA isolation. DNA is extracted from each well using the DNA minikit and collected as a 100-μL eluate. TaqMan real-time PCR-quantified 2-LTR junctions (2-LTR circles), late reverse transcription products, and integration junctions (Alu-LTR) are normalized to the level of host globin gene in each sample[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

449.38

Formula

C₂₁H₁₈F₃N₃O₅

CAS No.

1611493-60-7

SMILES

O=C1N([[email protected]](CC2)([H])C[[email protected]]2([H])O3)[[email protected]@]3([H])CN(C=C(C(NCC(C(F)=CC(F)=C4)=C4F)=O)C5=O)C1=C5O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Bictegravir
Cat. No.:
HY-17605
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Bictegravir

Cat. No.: HY-17605