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Elvitegravir Integrase inhibitor

Name: Elvitegravir
Brand: Selleck Chemicals
SKU: S2001
Availability: InStock
Rating: 5 (33 reviews)

Cat.No.S2001

Elvitegravir 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.

Chemical Structure

Molecular Weight: 447.88

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	Bacterial Antibiotics Anti-infection Fungal Antiviral COVID-19 Parasite Reverse Transcriptase HIV HCV Protease SARS-CoV HIV Protease Influenza Virus β-lactamase HBV CMV Neuraminidase HCV Thioredoxin Reductase HSV RSV Enterovirus 3C-Like Protease Ribosomal Peptidyl Transferase HPV
Related Products	MK-2048 BMS-707035 Robinetin Lavendustin B

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Activity Description
human C8166 cells	Function assay	Antiviral activity against HIV1 LAI 3B infected in human C8166 cells assessed as protection against virus-induced cytopathic effect by MTT assay, EC50=0.21 nM
MT4 cells	Function assay	Antiviral activity against HIV1 3B in MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.37 nM
human MT4 cells	Cytotoxicity assay	Cytotoxicity against human MT4 cells by MTT assay, CC50=1.15 μM
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	447.88	Formula	C₂₃H₂₃ClFNO₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	697761-98-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	GS-9137,JTK-303,D06677			Smiles	CC(C)C(CO)N1C=C(C(=O)C2=C1C=C(C(=C2)CC3=C(C(=CC=C3)Cl)F)OC)C(=O)O

Solubility

In vitro
Batch:

DMSO : 89 mg/mL (198.71 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 35 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (2.23mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, 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.

Mechanism of Action

Targets/IC₅₀/Ki	HIV-1 IIIB ^[1] (Cell-free assay) 0.7 nM HIV-2 ROD ^[1] (Cell-free assay) 1.4 nM HIV-2 EHO ^[1] (Cell-free assay) 2.8 nM
In vitro	Elvitegravir inhibits PBMC and PA with IC50 of 0.89 and 20 nM, respectively. This compound prevents the integration of HIV-1 cDNA through the inhibition of DNA strand transfer. It suppresses the replication of HIV-1, including various subtypes and multiple-drug-resistant clinical isolates, and HIV-2 strains with a 50% effective concentration in the subnanomolar to nanomolar range. This inhibitor blocks the replication of HIV-1 clinical isolates carrying NRTI, NNRTI, and PI resistance-associated genotypes. It inhibits the HIV replication at a step that occurs after reverse transcription but before proteolytic cleavage, consistent with the integration step. This chemical inhibits the synthesis of strand transfer products with an IC50 of 54 nM. It blocks integration via the inhibition of IN-mediated strand transfer. ^[1] This agent inhibits the integration of the HIV-based vector used as a positive control for the luciferase assay with an EC50 of 0.8 nM, as observed in the MAGI assay with HIV-1IIIB. It suppresses the replication of MLV infection with IC50 of 5.8 nM as well as that of the primate retrovirus SIV (IC50 = 0.5 nM), revealing that IN inhibitors have antiviral activity against a broad range of retroviruses. This compound is active against HIV-1 and HIV-2 and has a serum-free antiviral IC50 of 0.3-0.9 nM in peripheral blood mononuclear cells. ^[2]
References	[1] https://pubmed.ncbi.nlm.nih.gov/17977962/ [2] https://pubmed.ncbi.nlm.nih.gov/22149610/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04047420	Completed	HIV Infections	National Institute of Allergy and Infectious Diseases (NIAID)\|CONRAD	December 11 2019	Phase 1
NCT03976752	Completed	HIV/AIDS	Emory University\|Centers for Disease Control and Prevention	March 13 2019	Phase 1
NCT02985996	Completed	HIV Infections	Emory University\|Centers for Disease Control and Prevention	February 6 2017	Phase 1
NCT02251236	Completed	HIV	University of California San Diego\|Gilead Sciences\|University at Buffalo	January 2016	Not Applicable
NCT02600819	Completed	HIV-1 Infection	Gilead Sciences	December 14 2015	Phase 3
NCT02295384	Completed	HIV	Holdsworth House Medical Practice\|Gilead Sciences	November 2014	--

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