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.

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Biological Activity

Description

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

Targets

HIV-1 integrase ^[1]
()

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)

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

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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.

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Molarity Calculator

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

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Dilution Calculator

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

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The Serial Dilution Calculator Equation

Serial Dilutions
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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):

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Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2020-01-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04551573	Not yet recruiting	Drug: Rifapentine daily\|Drug: Rifapentine weekly	Tuberculosis\|Hiv	Yale University\|Gilead Sciences	November 2020	Phase 4
NCT04530630	Recruiting	Drug: BIKTARVY 50Mg-200Mg-25Mg Tablet	HIV Infections\|Renal Transplant Rejection	Weill Medical College of Cornell University\|Gilead Sciences	November 9 2020	Phase 4
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	Completed	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	--

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

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Integrase Signaling Pathway Map

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