BICTEGRAVIR | CAS 1611493-60-7

BICTEGRAVIR

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250mg	$1050	Check With Us
500mg	$1650	Check With Us
500mg	$2475	Check With Us

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Cat #: V3902 CAS #: 1611493-60-7 Purity ≥ 98%

Description: Bictegravir (formerly BIC; GS-9883; trade name: Biktarvy for the combination of bictegravir, embitcitabine, tenofovir alafenamide) is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase (IN) approved in 2018 for HIV treatment.

References: Tsiang M, et al. Antiviral Activity of Bictegravir (GS-9883), a Novel Potent HIV-1 Integrase Strand Transfer Inhibitor with an Improved Resistance Profile. Antimicrob Agents Chemother. 2016 Nov 21;60(12):7086-7097.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	449.37
Molecular Formula	C21H18F3N3O5
CAS No.	1611493-60-7
Storage	-20℃ for 3 years in powder formrr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: > 80 mg/mLrr
	Water: N/Arr
	Ethanol: N/A
SMILES Code	O=C(C1=CN(C2=C(O)C1=O)C[C@@]3([H])O[C@](C4)([H])CC[C@]4([H])N3C2=O)NCC5=C(F)C=C(F)C=C5 F
Synonyms	GS-9883; GS 9883; GS9883; GS-9883-01

Protocol	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.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	2.2253 mL	11.1267 mL	22.2534 mL	44.5068 mL
5mM	0.4451 mL	2.2253 mL	4.4507 mL	8.9014 mL
10mM	0.2225 mL	1.1127 mL	2.2253 mL	4.4507 mL
20mM	0.1113 mL	0.5563 mL	1.1127 mL	2.2253 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

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

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

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 µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.