Art. -Nr.: HY-14740

Elvitegravir

(Synonyms: GS-9137; JTK-303; D06677)

14 Cited Publications

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Based on 14 publication(s) in Google Scholar

Elvitegravir (GS-9137; JTK-303; D06677) 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, respectively.

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Reinheit: 99.90%
CAS. Nr.: 697761-98-1
Formel: C₂₃H₂₃ClFNO₅
Molecular Weight:447.88

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Elvitegravir Chemical Structure

CAS. Nr.: 697761-98-1

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Clinical Trial
Chemical Information
Publications (14)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
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Biologische Aktivität

Beschreibung

Elvitegravir (GS-9137; JTK-303; D06677) 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, respectively.

IC₅₀ & Target

HIV-1

HIV-2

Alle HIV Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
C8166	CC₅₀	17.2 μM Compound: Elvitegravir	Cytotoxicity against human C8166 cells by MTT assay Cytotoxicity against human C8166 cells by MTT assay	[PMID: 21763149]
C8166	EC₅₀	0.00021 μM Compound: Elvitegravir	Antiviral activity against HIV1 LAI 3B infected in human C8166 cells assessed as protection against virus-induced cytopathic effect by MTT assay Antiviral activity against HIV1 LAI 3B infected in human C8166 cells assessed as protection against virus-induced cytopathic effect by MTT assay	[PMID: 21763149]
C8166	EC₅₀	0.21 nM Compound: Elvitegravir	Antiviral activity against HIV1 LAI 3B infected in human C8166 cells assessed as protection against virus-induced cytopathic effect by MTT assay Antiviral activity against HIV1 LAI 3B infected in human C8166 cells assessed as protection against virus-induced cytopathic effect by MTT assay	[PMID: 21763149]
C8166	CC₅₀	17.2 μM Compound: 1	Cytotoxicity against human C8166 cells by MTT assay Cytotoxicity against human C8166 cells by MTT assay	[PMID: 21862337]
C8166	EC₅₀	0.001 μM Compound: 1	Antiviral activity against HIV1 A17 harboring reverse transcriptase Y181C mutant infected in human C8166 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay Antiviral activity against HIV1 A17 harboring reverse transcriptase Y181C mutant infected in human C8166 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	[PMID: 21862337]
C8166	EC₅₀	0.00021 μM Compound: 1	Antiviral activity against wild type HIV1 LAI-3B infected in human C8166 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay Antiviral activity against wild type HIV1 LAI-3B infected in human C8166 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	[PMID: 21862337]
C8166	EC₅₀	0.21 nM Compound: 1	Antiviral activity against wild type HIV1 LAI-3B infected in human C8166 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay Antiviral activity against wild type HIV1 LAI-3B infected in human C8166 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	[PMID: 21862337]
HEK-293T	CC₅₀	>250 μM Compound: Elvitegravir	Cytotoxicity against human HEK293T cells assessed as cell growth inhibition by MTT assay Cytotoxicity against human HEK293T cells assessed as cell growth inhibition by MTT assay	[PMID: 36898139]
HeLa	CC₅₀	>50 μM Compound: 1, EVG	Cytotoxicity against human HeLa cells expressing CD4-LTR-beta-gal after 24 hrs by ATPlite assay Cytotoxicity against human HeLa cells expressing CD4-LTR-beta-gal after 24 hrs by ATPlite assay	[PMID: 24684270]
HeLa	EC₅₀	0.0142 μM Compound: 1, EVG	Antiviral activity against HIV1 3B infected in human HeLa cells expressing CD4-LTR-beta-gal assessed as inhibition of viral replication after 3 days by reporter gene assay Antiviral activity against HIV1 3B infected in human HeLa cells expressing CD4-LTR-beta-gal assessed as inhibition of viral replication after 3 days by reporter gene assay	[PMID: 24684270]
HeLa	CC₅₀	>50 μM Compound: EVG	Cytotoxicity against human HeLa-CD4-LTR-beta-gal cells after 24 hrs by ATPlite reagent based luminescence analysis Cytotoxicity against human HeLa-CD4-LTR-beta-gal cells after 24 hrs by ATPlite reagent based luminescence analysis	[PMID: 25961960]
MT4	EC₅₀	0.9 nM Compound: 12	Antiviral activity against HIV1 3b in human MT4 cells Antiviral activity against HIV1 3b in human MT4 cells	[PMID: 16509568]
MT4	EC₅₀	1 nM Compound: GS-9137	Antiviral activity against vesicular stomatitis virus G-pseudotyped Human immunodeficiency virus infected in human MT-4 cells assessed as inhibition of viral replication Antiviral activity against vesicular stomatitis virus G-pseudotyped Human immunodeficiency virus infected in human MT-4 cells assessed as inhibition of viral replication	[PMID: 18160521]
MT4	EC₅₀	2 nM Compound: GS-9137	Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT-4 cells assessed as inhibition of viral replication Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT-4 cells assessed as inhibition of viral replication	[PMID: 18160521]
MT4	EC₅₀	0.001 μM Compound: GS-9137	Antiviral activity against HIV 1 3B infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay Antiviral activity against HIV 1 3B infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	[PMID: 18378713]
MT4	EC₅₀	0.012 μM Compound: GS-9137	Antiviral activity against HIV 1 NL4.3 integrase E92Q mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay Antiviral activity against HIV 1 NL4.3 integrase E92Q mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	[PMID: 18378713]
MT4	EC₅₀	0.015 μM Compound: GS-9137	Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 20 passages selected in presence of compound Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 20 passages selected in presence of compound	[PMID: 18378713]
MT4	EC₅₀	0.018 μM Compound: GS-9137	Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 40 passages selected in presence of compound Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 40 passages selected in presence of compound	[PMID: 18378713]
MT4	EC₅₀	0.033 μM Compound: GS-9137	Antiviral activity against HIV 1 3B harboring integrase E92Q S230N double mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 20 passages in presence of compound Antiviral activity against HIV 1 3B harboring integrase E92Q S230N double mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 20 passages in presence of compound	[PMID: 18378713]
MT4	EC₅₀	0.05 μM Compound: GS-9137	Antiviral activity against HIV 1 3B harboring integrase L34M mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 40 passages in presence of compound Antiviral activity against HIV 1 3B harboring integrase L34M mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 40 passages in presence of compound	[PMID: 18378713]
MT4	EC₅₀	0.059 μM Compound: GS-9137	Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 60 passages selected in presence of compound Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 60 passages selected in presence of compound	[PMID: 18378713]
MT4	EC₅₀	0.077 μM Compound: GS-9137	Antiviral activity against HIV 1 3B harboring integrase E92Q, S230N and L34M triple mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 60 passages in presence of compound Antiviral activity against HIV 1 3B harboring integrase E92Q, S230N and L34M triple mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 60 passages in presence of compound	[PMID: 18378713]
MT4	EC₅₀	0.0006 μM Compound: GS-9137	Antiviral activity against HIV 1 NL4.3 harboring integrase L74M mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay Antiviral activity against HIV 1 NL4.3 harboring integrase L74M mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	[PMID: 18378713]
MT4	EC₅₀	0.0007 μM Compound: GS-9137	Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	[PMID: 18378713]
MT4	EC₅₀	0.0009 μM Compound: GS-9137	Antiviral activity against HIV 1 NL4.3 integrase S230N mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay Antiviral activity against HIV 1 NL4.3 integrase S230N mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	[PMID: 18378713]
MT4	EC₅₀	0.6 nM Compound: GS-9137	Antiviral activity against HIV 1 NL4.3 harboring integrase L74M mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay Antiviral activity against HIV 1 NL4.3 harboring integrase L74M mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	[PMID: 18378713]
MT4	EC₅₀	0.7 nM Compound: GS-9137	Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	[PMID: 18378713]
MT4	EC₅₀	0.9 nM Compound: GS-9137	Antiviral activity against HIV 1 NL4.3 integrase S230N mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay Antiviral activity against HIV 1 NL4.3 integrase S230N mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	[PMID: 18378713]
MT4	CC₅₀	2.12 μM Compound: 1, GS-9137	Cytotoxicity against human MT4 cells Cytotoxicity against human MT4 cells	[PMID: 18417342]
MT4	EC₅₀	0.0008 μM Compound: 1, GS-9137	Antiviral activity against HIV1 3B assessed as inhibition of viral-induced cytopathic effect in human MT4 cells Antiviral activity against HIV1 3B assessed as inhibition of viral-induced cytopathic effect in human MT4 cells	[PMID: 18417342]
MT4	EC₅₀	0.8 nM Compound: 1, GS-9137	Antiviral activity against HIV1 3B assessed as inhibition of viral-induced cytopathic effect in human MT4 cells Antiviral activity against HIV1 3B assessed as inhibition of viral-induced cytopathic effect in human MT4 cells	[PMID: 18417342]
MT4	CC₅₀	2.12 μM Compound: GS-9137	Cytotoxicity against human MT4 cells by MTT assay Cytotoxicity against human MT4 cells by MTT assay	[PMID: 18541726]
MT4	EC₅₀	0.00083 μM Compound: GS-9137	Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of viral replication Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of viral replication	[PMID: 18541726]
MT4	EC₅₀	0.83 nM Compound: GS-9137	Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of viral replication Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of viral replication	[PMID: 18541726]
MT4	CC₅₀	1.15 μM Compound: 2, elvitegravir, GS-9137	Cytotoxicity against human MT4 cells by MTT assay Cytotoxicity against human MT4 cells by MTT assay	[PMID: 18665580]
MT4	EC₅₀	0.00037 μM Compound: 2, elvitegravir, GS-9137	Antiviral activity against HIV1 3B in MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay Antiviral activity against HIV1 3B in MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	[PMID: 18665580]
MT4	EC₅₀	0.37 nM Compound: 2, elvitegravir, GS-9137	Antiviral activity against HIV1 3B in MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay Antiviral activity against HIV1 3B in MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	[PMID: 18665580]
MT4	CC₅₀	4 μM Compound: 49	Cytotoxicity against human MT4 cells after 5 days by MTT assay Cytotoxicity against human MT4 cells after 5 days by MTT assay	[PMID: 19719237]
MT4	EC₅₀	0.9 μM Compound: 49	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay	[PMID: 19719237]
MT4	EC₅₀	11.6 nM Compound: EVG	Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect	[PMID: 20479206]
MT4	EC₅₀	2.12 μM Compound: 2, GS-9137	Cytotoxicity against human MT4 cells by MTT assay Cytotoxicity against human MT4 cells by MTT assay	[PMID: 20630765]
MT4	EC₅₀	0.0008 μM Compound: 2, GS-9137	Antiviral activity against HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect Antiviral activity against HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect	[PMID: 20630765]
MT4	EC₅₀	0.8 nM Compound: 2, GS-9137	Antiviral activity against HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect Antiviral activity against HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect	[PMID: 20630765]
MT4	CC₅₀	2.12 μM Compound: 1, GS-9137	Cytotoxicity against human MT4 cells by MTT assay Cytotoxicity against human MT4 cells by MTT assay	[PMID: 21227550]
MT4	EC₅₀	0.0008 μM Compound: 1, GS-9137	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	[PMID: 21227550]
MT4	EC₅₀	0.8 nM Compound: 1, GS-9137	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	[PMID: 21227550]
MT4	IC₅₀	1.3 nM Compound: EVG	Inhibition of wild type HIV1 3B infected in human MT4 cells using cells pre-incubated with compound for 1 hr measured 4 days post viral infection by MTT assay Inhibition of wild type HIV1 3B infected in human MT4 cells using cells pre-incubated with compound for 1 hr measured 4 days post viral infection by MTT assay	[PMID: 22963135]
MT4	IC₅₀	29 nM Compound: EVG	Inhibition of wild type HIV1 3B infected in human MT4 cells using cells pre-incubated with compound for 1 hr measured 4 days post viral infection in presence of 20 mg/ml HSA by MTT assay Inhibition of wild type HIV1 3B infected in human MT4 cells using cells pre-incubated with compound for 1 hr measured 4 days post viral infection in presence of 20 mg/ml HSA by MTT assay	[PMID: 22963135]
MT4	CC₅₀	4.6 μM Compound: 3, EVG	Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay	[PMID: 25907370]
MT4	EC₅₀	0.0022 μM Compound: 3, EVG	Antiviral activity against HIV1 harboring K103N/Y181C double mutant infected in human MT4 cells assessed as protection of cells from virus-induced cytopathic after 5 days by MTT assay Antiviral activity against HIV1 harboring K103N/Y181C double mutant infected in human MT4 cells assessed as protection of cells from virus-induced cytopathic after 5 days by MTT assay	[PMID: 25907370]
MT4	EC₅₀	0.0031 μM Compound: 3, EVG	Antiviral activity against wild-type HIV1 3B infected in human MT4 cells assessed as protection of cells from virus-induced cytopathic after 5 days by MTT assay Antiviral activity against wild-type HIV1 3B infected in human MT4 cells assessed as protection of cells from virus-induced cytopathic after 5 days by MTT assay	[PMID: 25907370]
MT4	CC₅₀	6.3 μM Compound: EVG	Cytotoxic activity against mock-infected human MT4 cellls assessed as reduction in cell viability by MTT assay Cytotoxic activity against mock-infected human MT4 cellls assessed as reduction in cell viability by MTT assay	[PMID: 28951095]

In Vitro

Elvitegravir (GS-9137; JTK-303; D06677) blocks the integration of HIV-1 cDNA through the inhibition of DNA strand transfer. Elvitegravir exerts potent anti-HIV activity against not only wild-type strains but also drug-resistant clinical isolates. Interestingly, Elvitegravir also shows antiviral activity against murine leukemia virus (MLV) and simian immunodeficiency virus (SIV). Elvitegravir shows potent antiviral activity against three laboratory strains of HIV, with EC₅₀ values in the subnanomolar to nanomolar range. Next, the activity of Elvitegravir is evaluated against wild-type clinical isolates representing various subtypes of HIV-1. Elvitegravir suppresses the replication of all HIV-1 subtypes tested, with an antiviral EC₅₀ ranging from 0.1 to 1.26 nM. Moreover, Elvitegravir suppresses the replication of HIV-1 clinical isolates carrying NRTI, NNRTI, and PI resistance-associated genotypes, as did a control IN inhibitor, the compound L-870,810. The cytotoxicities of these inhibitors are also determined using an MTT colorimetric assay. Mean values for the concentration that suppresses the viability of target cells by 50% for Elvitegravir and L-870,810 in PBMC obtained from three independent donors are 4.6±0.5 μM and 2.7±0.6 μM, respectively. Thus, Elvitegravir can suppress various HIV strains, including diverse HIV-1 subtypes and clinical isolates carrying multiple mutations associated with resistance to currently approved antiretroviral drugs^[1].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 697761-98-1
Appearance Solid
Molecular Weight 447.88
Formel C₂₃H₂₃ClFNO₅
Color White to off-white
SMILES

O=C(O)C1=CN(C2=C(C1=O)C=C(C(OC)=C2)CC3=CC=CC(Cl)=C3F)[C@@H](C(C)C)CO
Synonyms

GS-9137; JTK-303; D06677
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (14)

All Cell Proliferation/Viability Assay

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Journal Impact Factor

Nat Cell Biol

A continuous totipotent-like cell-based embryo model recapitulates mouse embryogenesis from zygotic genome activation to gastrulation. [Abstract]

2025 Oct 15. PMID: 41094030
J Neuroimmune Pharmacol

Antiretroviral Drugs Promote Amyloidogenesis by De-Acidifying Endolysosomes. [Abstract]

2021 Mar;16(1):159-168. PMID: 31338753
Int J Antimicrob Agents

Efficacy of antiretroviral compounds against Toxoplasma gondii in vitro. [Abstract]

2019 Dec;54(6):814-819. PMID: 31479744
RSC Med Chem

Structure-guided design of a methyltransferase-like 3 (METTL3) proteolysis targeting chimera (PROTAC) incorporating an indole-nicotinamide chemotype. [Abstract]

2025 Jun 19. PMID: 40599585
Antiviral Res

Discovery of 4-oxoquinolines, a new chemical class of anti-HIV-1 compounds. [Abstract]

2019 Feb:162:101-109. PMID: 30582937
Antimicrob Agents Chemother

Effects of Antiviral Drugs on Organic Anion Transport in Human Placental BeWo Cells. [Abstract]

2015 Dec;59(12):7666-70. PMID: 26416870

Elvitegravir purchased from MedChemExpress. Usage Cited in: Antimicrob Agents Chemother. 2015 Dec;59(12):7666-70. [Abstract]

Effects of antiviral drugs on cellular uptake of fluorescein by BeWo cells. The cells are incubated with 1 μM fluorescein in the presence of 100 μM compounds for 10 min at 37°C.
Microb Pathog

Antibiotic discovery against Piscirickettsia salmonis using a combined in silico and in vitro approach. [Abstract]

2023 Jul:180:106122. PMID: 37094756
Open Forum Infect Dis

Novel Dolutegravir and Lenacapavir Resistance Patterns in Human Immunodeficiency Virus Type 2 Infection: A Case Report. [Abstract]

2024 Nov 29;12(1):ofae705. PMID: 39741997
Toxicol Appl Pharmacol

The inhibitory effect of antiretroviral drugs on the L-carnitine uptake in human placenta. [Abstract]

2019 Apr 1:368:18-25. PMID: 30735677
Cell Physiol Biochem

Stimulating Effect of Elvitegravir on Suicidal Erythrocyte Death. [Abstract]

2016;38(3):1111-20. PMID: 26963694

Elvitegravir purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2016;38(3):1111-20. [Abstract]

Arithmetic means±SEM (n=10) of erythrocyte annexin-V-binding following incubation for 48 hours to Ringer solution without (white bar) or with (black bars) Elvitegravir (0.5-2.5 µg/mL).
J Spectrosc (Hindawi)

2015 (2015), Article ID 435674, 9 pages.
bioRxiv

2026 Apr 21.
Preprints

2024 Apr 23.
PeerJ Physical Chemistry

2019, 1:e6.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 175 mg/mL (390.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2327 mL

11.1637 mL

22.3274 mL

5 mM

0.4465 mL

2.2327 mL

4.4655 mL

10 mM

0.2233 mL

1.1164 mL

2.2327 mL

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. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (5.58 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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.

Protocol 2

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

Solubility: ≥ 2.08 mg/mL (4.64 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.64 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[1]

MT-2 cells (2×10⁵ cells) are infected with HIV-1_IIIB and then cultured in the presence of 0.5 nM or 0.1 nM Elvitegravir. Cultures are incubated at 37°C until an extensive cytopathic effect (CPE) is observed, and the culture supernatant is then harvested for further passage in fresh MT-2 cells. The concentration of Elvitegravir is increased when a significant CPE is observed. At the indicated passages, proviral DNA is extracted from infected MT-2 cells and then subjected to PCR, followed by direct population-based sequencing. Susceptibility to Elvitegravir at the indicated passages is determined using the MAGI assay or p24 production^[1].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Shimura K, et al. Broad antiretroviral activity and resistance profile of the novel human immunodeficiency virus integrase inhibitor elvitegravir (JTK-303/GS-9137). J Virol. 2008 Jan;82(2):764-74. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. 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	2.2327 mL	11.1637 mL	22.3274 mL	55.8185 mL
	5 mM	0.4465 mL	2.2327 mL	4.4655 mL	11.1637 mL
	10 mM	0.2233 mL	1.1164 mL	2.2327 mL	5.5819 mL
	15 mM	0.1488 mL	0.7442 mL	1.4885 mL	3.7212 mL
	20 mM	0.1116 mL	0.5582 mL	1.1164 mL	2.7909 mL
	25 mM	0.0893 mL	0.4465 mL	0.8931 mL	2.2327 mL
	30 mM	0.0744 mL	0.3721 mL	0.7442 mL	1.8606 mL
	40 mM	0.0558 mL	0.2791 mL	0.5582 mL	1.3955 mL
	50 mM	0.0447 mL	0.2233 mL	0.4465 mL	1.1164 mL
	60 mM	0.0372 mL	0.1861 mL	0.3721 mL	0.9303 mL
	80 mM	0.0279 mL	0.1395 mL	0.2791 mL	0.6977 mL
	100 mM	0.0223 mL	0.1116 mL	0.2233 mL	0.5582 mL

Elvitegravir

14 Cited Publications

100 mg Angebot einholen

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Elvitegravir

Anti-Infection Compound Library

Metabolism/Protease Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Antiviral Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Off-patent Drug Library

Metabolic Enzyme Compound Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Elvitegravir

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Elvitegravir

Anti-Infection Compound Library

Metabolism/Protease Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Antiviral Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Off-patent Drug Library

Metabolic Enzyme Compound Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Elvitegravir

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Elvitegravir Related Classifications

HY-14740 Related Classifications