Bictegravir

Name: Bictegravir
Brand: Selleck Chemicals
SKU: S5911
Rating: 5 (0 reviews)

For research use only.

Catalog No.S5911 Synonyms: GS-9883

CAS No. 1611493-60-7

Bictegravir is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase.

Purity & Quality Control

Choose Selective Integrase Inhibitors

Biological Activity

Description

Bictegravir is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase.

In vitro

Bictegravir exhibits potent and selective in vitro antiretroviral activity in both T-cell lines and primary human T lymphocytes, with 50% effective concentrations ranging from 1.5 to 2.4 nM and selectivity indices up to 8,700 relative to cytotoxicity. Bictegravir 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 integrase, with an IC50 of 241 ± 51 nM. Bictegravir potently inhibits HIV-1 replication in both MT-2 and MT-4 cells with EC50s of 1.5 and 2.4 nM, respectively, and selectivity indices (50% cytotoxic concentration [CC50]/EC50) of ∼6,800 in MT-2 cells and ∼1,500 in MT-4 cells^[1].

Protocol

References

[1] Tsiang M, et al. Antimicrob Agents Chemother. 2016, 60(12):7086-7097.

Solubility (25°C)

In vitro	DMSO	90 mg/mL (200.27 mM)
	Water	Insoluble
	Ethanol	Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight	449.38
Formula	C₂₁H₁₈F₃N₃O₅
CAS No.	1611493-60-7
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	GS-9883
Smiles	C1CC2CC1N3C(O2)CN4C=C(C(=O)C(=C4C3=O)O)C(=O)NCC5=C(C=C(C=C5F)F)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% DMSO+ % + % Tween 80+ % ddH₂O

Calculate Reset

Calculation results:

Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2020-09-01)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04530630	Not yet recruiting	Drug: BIKTARVY 50Mg-200Mg-25Mg Tablet	HIV Infections\|Renal Transplant Rejection	Weill Medical College of Cornell University\|Gilead Sciences	September 2020	Phase 3
NCT03858478	Recruiting	Drug: Biktarvy arm	HIV Seropositivity	Institut de Médecine et d''Epidémiologie Appliquée - Fondation Internationale Léon M''Ba	November 18 2019	Phase 4
NCT03789968	Enrolling by invitation	Drug: bictegravir/emtricitabine/tenofovir alafenamide	HIV/AIDS	Thomas Jefferson University\|University of Maryland College Park\|Indiana University Health\|The Brooklyn Hospital Center\|University of Illinois at Chicago\|Nova Southeastern University\|University of California San Francisco	September 1 2019	--
NCT02881320	Active not recruiting	Drug: B/F/TAF (Adult Strength)\|Drug: B/F/TAF (Low Dose)	HIV-1 Infection	Gilead Sciences	September 21 2016	Phase 2\|Phase 3
NCT02400307	Completed	Drug: Bictegravir	HIV	Gilead Sciences	April 17 2015	Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Integrase Signaling Pathway Map

Related Integrase Products

Cabotegravir (GSK1265744) ^New

Cabotegravir (GSK744, GSK1265744) is a long-acting HIV integrase inhibitor against a broad range of HIV subtypes, and inhibits the HIV-1 integrase catalyzed strand transfer reaction with IC50 of 3.0 nM. Phase 2.
Tenofovir Alafenamide (GS-7340) ^New

Tenofovir Alafenamide (GS-7340) is a prodrug of tenofovir, which is a reverse transcriptase inhibitor, used to treat HIV and Hepatitis B.
Elvitegravir (JTK-303)

Elvitegravir (GS-9137, JTK-303) is an HIV integrase inhibitor for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM in cell-free assays, respectively.
Raltegravir (MK-0518)

Raltegravir (MK-0518) is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM in cell-free assays, respectively. It shows greater than 1000-fold selectivity for HIV-1 IN over several related Mg2+-dependent enzyme such as HCV polymerase, HIV reverse transcriptase, HIV RNaseH and human α-, β-, γ-polymerases.

Features:The 1st approved human immunodeficiency virus type 1 (HIV-1) integrase inhibitor.
BMS-707035

BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM. Phase 2.
Dolutegravir (GSK1349572)

Dolutegravir (GSK1349572, S/GSK1349572) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM in a cell-free assay, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.

Features:A next-generation and two-metal-binding HIV integrase strand transfer inhibitor.
MK-2048

MK-2048 is a potent inhibitor of integrase (IN) and IN_R263K with IC50 of 2.6 nM and 1.5 nM, respectively.
Maraviroc

Maraviroc (UK-427857) is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM in cell-free assays, respectively. Maraviroc is used in the treatment of HIV infection.
Tenofovir Disoproxil Fumarate

Tenofovir (GS-1278) Disoproxil Fumarate belongs to a class of antiretroviral drugs, it inhibits the activity of HIV reverse transcriptase by competing with the natural substrate deoxyadenosine 5’-triphosphate and, after incorporation into DNA, by DNA chain termination.

Choose Your Country or Region

By Signaling Pathways

By product type