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

Bictegravir  (Synonyms: GS-9883)

Cat. No.: HY-17605 Purity: 99.79%
COA Handling Instructions

Bictegravir (GS-9883) is a 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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 76 In-stock
Solution
10 mM * 1 mL in DMSO USD 76 In-stock
Solid
1 mg USD 55 In-stock
5 mg USD 77 In-stock
10 mg USD 132 In-stock
25 mg USD 267 In-stock
50 mg USD 400 In-stock
100 mg USD 640 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Bictegravir:

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.

IC50 & Target

HIV-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].

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

Clinical Trial
Molecular Weight

449.38

Formula

C21H18F3N3O5

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 83.3 mg/mL (185.37 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.56 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.56 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.79%

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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2253 mL 11.1264 mL 22.2529 mL 55.6322 mL
5 mM 0.4451 mL 2.2253 mL 4.4506 mL 11.1264 mL
10 mM 0.2225 mL 1.1126 mL 2.2253 mL 5.5632 mL
15 mM 0.1484 mL 0.7418 mL 1.4835 mL 3.7088 mL
20 mM 0.1113 mL 0.5563 mL 1.1126 mL 2.7816 mL
25 mM 0.0890 mL 0.4451 mL 0.8901 mL 2.2253 mL
30 mM 0.0742 mL 0.3709 mL 0.7418 mL 1.8544 mL
40 mM 0.0556 mL 0.2782 mL 0.5563 mL 1.3908 mL
50 mM 0.0445 mL 0.2225 mL 0.4451 mL 1.1126 mL
60 mM 0.0371 mL 0.1854 mL 0.3709 mL 0.9272 mL
80 mM 0.0278 mL 0.1391 mL 0.2782 mL 0.6954 mL
100 mM 0.0223 mL 0.1113 mL 0.2225 mL 0.5563 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Bictegravir
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