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Raltegravir

(Synonyms: MK-0518)

27 Cited Publications

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Based on 27 publication(s) in Google Scholar

Raltegravir is a potent integrase (IN) inhibitor, used to treat HIV infection.

For research use only. We do not sell to patients.

Purity: 99.82%
CAS No.: 518048-05-0
Formula: C₂₀H₂₁FN₆O₅
Molecular Weight:444.42

Storage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Raltegravir Chemical Structure

CAS No.: 518048-05-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (27)
Solvent & Solubility
- In Vitro
- In Vivo
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Purity & Documentation
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Biological Activity

Description

Raltegravir is a potent integrase (IN) inhibitor, used to treat HIV infection.

IC₅₀ & Target

HIV-1

HIV-2

All HIV Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CEM-SS	CC₅₀	>10 μM Compound: 1	Cytotoxicity against human CEM-SS cells assessed as cell death after 6 days by MTS assay Cytotoxicity against human CEM-SS cells assessed as cell death after 6 days by MTS assay	[PMID: 27283261]
CHO	IC₅₀	246.7 μM Compound: raltegravir	Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits	[PMID: 23812503]
HEK293	IC₅₀	170 μM Compound: Raltegravir	Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method	[PMID: 21030469]
HEK293	IC₅₀	190 μM Compound: Raltegravir	Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method	[PMID: 21030469]
HeLa	IC₅₀	>100 μM Compound: Raltegravir	Cytotoxicity against human HeLa cells by MTT assay Cytotoxicity against human HeLa cells by MTT assay	[PMID: 22858300]
HeLa	IC₅₀	0.01 μM Compound: Raltegravir	Antiviral activity against VSV-G pseudotyped HIV1 lentiviral particles infected in human HeLa cells incubated for 48 hrs by spectrofluorometry Antiviral activity against VSV-G pseudotyped HIV1 lentiviral particles infected in human HeLa cells incubated for 48 hrs by spectrofluorometry	[PMID: 22858300]
HeLa	CC₅₀	>250 μM Compound: 1	Cytotoxicity against human HeLa cells expressing CD4 after 24 hrs by beta-galactosidase reporter gene assay Cytotoxicity against human HeLa cells expressing CD4 after 24 hrs by beta-galactosidase reporter gene assay	[PMID: 24124919]
HeLa	EC₅₀	24 nM Compound: 1	Antiviral activity against HIV1 3B infected in human HeLa cells expressing CD4 assessed as inhibition of viral replication after 2 days by beta-galactosidase reporter gene assay Antiviral activity against HIV1 3B infected in human HeLa cells expressing CD4 assessed as inhibition of viral replication after 2 days by beta-galactosidase reporter gene assay	[PMID: 24124919]
HeLa	CC₅₀	>50 μM Compound: 2, RAL, MK-0518	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	0.0236 μM Compound: 2, RAL, MK-0518	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	>250 μM Compound: 1	Cytotoxicity against human HeLa expressing CD4 and integrated copy of HIV-1 LTR-driven beta-D-galactosidase reporter cells after 24 hrs by luminescence assay Cytotoxicity against human HeLa expressing CD4 and integrated copy of HIV-1 LTR-driven beta-D-galactosidase reporter cells after 24 hrs by luminescence assay	[PMID: 25629256]
HeLa	CC₅₀	>50 μM Compound: 1	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]
HOS	EC₅₀	0.004 μM Compound: 1	Antiviral activity against HIV1 harboring wild-type integrase infected in human HOS cells Antiviral activity against HIV1 harboring wild-type integrase infected in human HOS cells	[PMID: 21493066]
HOS	CC₅₀	>100 μM Compound: 1, RAL	Cytotoxicity against HOS cells assessed as reduction in ATP level after 48 hrs by luciferase reporter gene assay Cytotoxicity against HOS cells assessed as reduction in ATP level after 48 hrs by luciferase reporter gene assay	[PMID: 24471816]
HOS	EC₅₀	154 nM Compound: 1, RAL	Antiviral activity against Human immunodeficiency virus 1 harboring integrase N155H mutant infected in HOS cells preincubated for 3 hrs followed by viral infection measured after 48 hrs by luciferase reporter gene assay Antiviral activity against Human immunodeficiency virus 1 harboring integrase N155H mutant infected in HOS cells preincubated for 3 hrs followed by viral infection measured after 48 hrs by luciferase reporter gene assay	[PMID: 24471816]
HOS	EC₅₀	162 nM Compound: 1, RAL	Antiviral activity against Human immunodeficiency virus 1 harboring integrase Y143R mutant infected in HOS cells preincubated for 3 hrs followed by viral infection measured after 48 hrs by luciferase reporter gene assay Antiviral activity against Human immunodeficiency virus 1 harboring integrase Y143R mutant infected in HOS cells preincubated for 3 hrs followed by viral infection measured after 48 hrs by luciferase reporter gene assay	[PMID: 24471816]
HOS	EC₅₀	1900 nM Compound: 1, RAL	Antiviral activity against Human immunodeficiency virus 1 harboring integrase G140S/Q148H double mutant infected in HOS cells preincubated for 3 hrs followed by viral infection measured after 48 hrs by luciferase reporter gene assay Antiviral activity against Human immunodeficiency virus 1 harboring integrase G140S/Q148H double mutant infected in HOS cells preincubated for 3 hrs followed by viral infection measured after 48 hrs by luciferase reporter gene assay	[PMID: 24471816]
HOS	EC₅₀	4 nM Compound: 1, RAL	Antiviral activity against wild-type Human immunodeficiency virus 1 infected in HOS cells preincubated for 3 hrs followed by viral infection measured after 48 hrs by luciferase reporter gene assay Antiviral activity against wild-type Human immunodeficiency virus 1 infected in HOS cells preincubated for 3 hrs followed by viral infection measured after 48 hrs by luciferase reporter gene assay	[PMID: 24471816]
Jurkat	CC₅₀	>120 μM Compound: RAL; MK-0518	Cytotoxicity against human Jurkat cells after 48 to 72 hrs by MTT assay Cytotoxicity against human Jurkat cells after 48 to 72 hrs by MTT assay	[PMID: 26487913]
MT2	EC₅₀	16 nM Compound: 1, raltegravir	Antiviral activity against HIV in MT2 cells in presence of 35 mg/mL human serum albumin Antiviral activity against HIV in MT2 cells in presence of 35 mg/mL human serum albumin	[PMID: 18207398]
MT2	EC₅₀	6 nM Compound: 1, raltegravir	Antiviral activity against HIV1 3B in MT2 cells after 5 days Antiviral activity against HIV1 3B in MT2 cells after 5 days	[PMID: 18207398]
MT2	EC₅₀	18 nM Compound: MK-0518	Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS, HSA and alpha1-AGP Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS, HSA and alpha1-AGP	[PMID: 19104010]
MT2	EC₅₀	3 nM Compound: MK-0518	Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS	[PMID: 19104010]
MT2	CC₅₀	>100000 nM Compound: MK-0518	Cytotoxicity against human MT2 cells infected with HIV1 3B by three fold dilution method in presence of 10% FBS Cytotoxicity against human MT2 cells infected with HIV1 3B by three fold dilution method in presence of 10% FBS	[PMID: 19104010]
MT2	EC₅₀	20 nM Compound: 1, MK-0518	Antiviral activity against HIV1 3B infected in human MT2 cells after 5 days by chemiluminescence in presence of human serum albumin Antiviral activity against HIV1 3B infected in human MT2 cells after 5 days by chemiluminescence in presence of human serum albumin	[PMID: 19285389]
MT2	EC₅₀	4 nM Compound: 1, MK-0518	Antiviral activity against HIV1 3B infected in human MT2 cells after 5 days by chemiluminescence in presence of fetal bovine serum Antiviral activity against HIV1 3B infected in human MT2 cells after 5 days by chemiluminescence in presence of fetal bovine serum	[PMID: 19285389]
MT4	EC₅₀	1.8 nM Compound: MK-0518	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	2 nM Compound: MK-0518	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	0.006 μM Compound: MK-0518	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	0.007 μM Compound: MK-0518	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	0.009 μM Compound: MK-0518	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	0.01 μM Compound: MK-0518	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	0.015 μM Compound: MK-0518	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	0.025 μM Compound: MK-0518	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	0.068 μM Compound: MK-0518	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	CC₅₀	>18 μM Compound: 2, MK-0518	Cytotoxicity against human MT4 cells Cytotoxicity against human MT4 cells	[PMID: 18417342]
MT4	EC₅₀	0.013 μM Compound: 2, MK-0518	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	>18 μM Compound: MK-0518	Cytotoxicity against human MT4 cells by MTT assay Cytotoxicity against human MT4 cells by MTT assay	[PMID: 18541726]
MT4	EC₅₀	0.0014 μM Compound: MK-0518	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	58200 nM Compound: MK-0518	Cytotoxicity against human MT4 cells infected with HIV1 3B by three fold dilution method in presence of 10% FBS Cytotoxicity against human MT4 cells infected with HIV1 3B by three fold dilution method in presence of 10% FBS	[PMID: 19104010]
MT4	EC₅₀	8 nM Compound: MK-0518	Antiviral activity against HIV1 3B infected in human MT-4 cells by two fold dilution method in presence of 10% FBS Antiviral activity against HIV1 3B infected in human MT-4 cells by two fold dilution method in presence of 10% FBS	[PMID: 19104010]
MT4	CC₅₀	142.73 μM Compound: MK-0518	Cytotoxicity against human MT4 cells by MTT method Cytotoxicity against human MT4 cells by MTT method	[PMID: 19447621]
MT4	EC₅₀	0.0064 μM Compound: MK-0518	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathogenicity by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathogenicity by MTT assay	[PMID: 19447621]
MT4	EC₅₀	6.1 nM Compound: RAL	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	>18 μM Compound: 1, MK-0518	Cytotoxicity against human MT4 cells by MTT assay Cytotoxicity against human MT4 cells by MTT assay	[PMID: 20630765]
MT4	EC₅₀	0.013 μM Compound: 1, MK-0518	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	>18 μM Compound: 2, MK-0518	Cytotoxicity against human MT4 cells by MTT assay Cytotoxicity against human MT4 cells by MTT assay	[PMID: 21227550]
MT4	EC₅₀	0.013 μM Compound: 2, MK-0518	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	29 nM Compound: RAL	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	IC₅₀	6.2 nM Compound: RAL	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	EC₅₀	0.016 μM Compound: 1	Antiviral activity against HIV1 3B/LAI infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect measured survival after 5 days by MTT assay Antiviral activity against HIV1 3B/LAI infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect measured survival after 5 days by MTT assay	[PMID: 24124919]
MT4	CC₅₀	>8 μM Compound: Raltegravir	Cytotoxicity against human MT4 cells infected with HIV-1 3B assessed as reduction in cell viability by MTT assay Cytotoxicity against human MT4 cells infected with HIV-1 3B assessed as reduction in cell viability by MTT assay	[PMID: 24793360]
MT4	EC₅₀	0.006 μM Compound: Raltegravir	Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay	[PMID: 24793360]
MT4	CC₅₀	>8 μM Compound: Isentress	Cytotoxicity against human MT4 cells by MTT assay Cytotoxicity against human MT4 cells by MTT assay	[PMID: 24900718]
MT4	EC₅₀	0.006 μM Compound: Isentress	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: 24900718]
MT4	CC₅₀	>55.8 μM Compound: RAL	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]
MT4	CC₅₀	>56.25 μM Compound: RAL	Cytotoxicity against human MT4 cells after 5 days by MTT assay Cytotoxicity against human MT4 cells after 5 days by MTT assay	[PMID: 29940462]
MT4	CC₅₀	6.51 μM Compound: RAL	Cytotoxicity in mock-infected human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay Cytotoxicity in mock-infected human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay	[PMID: 31324562]
TZM	CC₅₀	>30 μM Compound: Raltegravir	Cytotoxicity against human TZM-bl cells after 48 hrs by MTT assay Cytotoxicity against human TZM-bl cells after 48 hrs by MTT assay	[PMID: 22154762]
TZM	CC₅₀	855.6 μM Compound: Raltegravir	Cytotoxicity against human TZM-bl cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human TZM-bl cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 24291042]
TZM	CC₅₀	>200 μM Compound: RAL; MK-0518	Cytotoxicity against human TZM-bl cells after 48 hrs by Cell-titerGlo assay Cytotoxicity against human TZM-bl cells after 48 hrs by Cell-titerGlo assay	[PMID: 26487913]

In Vitro

PFV IN carrying the S217H substitution is 10-fold less susceptible to Raltegravir with IC₅₀ of 900 nM. PFV IN displays 10% of WT activity and is inhibited by Raltegravir with an IC₅₀ of 200 nM, indicating a appr twofold decrease in susceptibility to the IN strand transfer inhibitor (INSTI) compared with WT IN. S217Q PFV IN is as sensitive to Raltegravir as the WT enzyme^[1]. Raltegravir is metabolized by glucuronidation, not hepatically. Raltegravir has potent in vitro activity against HIV-1, with a 95% inhibitory concentration of 31±20 nM, in human T lymphoid cell cultures. Raltegravir is also active against HIV-2 when Raltegravir is tested in CEMx174 cells, with an IC₉₅of 6 nM. Raltegravir metabolism occurs primarily through glucuronidation. Drugs that are strong inducers of the glucuronidation enzyme, UGT1A1, significantly reduce Raltegravir concentrations and should not be used. Raltegravir exhibits weak inhibitory effects on hepatic cytochrome P450 activity. Raltegravir does not induce CYP3A4 RNA expression or CYP3A4-dependent testosterone 6-β-hydroxylase activity^[2]. Raltegravir cellular permeativity is reduced in the presence of magnesium and calcium^[3]. Raltegravir and related HIV-1 integrase (IN) strand transfer inhibitors (INSTIs efficiently block viral replication^[4]. In acutely infected human lymphoid CD4⁺ T-cell lines MT-4 and CEMx174, SIVmac251 replication is efficiently inhibited by Raltegravir, which shows an EC₉₀ in the low nanomolar range^[5].

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

In Vivo

Raltegravir induces viro-immunological improvement of nonhuman primates with progressing SIVmac251 infection. One non-human primate shows an undetectable viral load following Raltegravir monotherapy^[5].

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

Chemical Information

CAS No. 518048-05-0
Appearance Solid
Molecular Weight 444.42
Formula C₂₀H₂₁FN₆O₅
Color White to off-white
SMILES

O=C(C(O)=C(C(NCC1=CC=C(C=C1)F)=O)N=C2C(C)(C)NC(C3=NN=C(C)O3)=O)N2C
Synonyms

MK-0518
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (27)

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Journal Impact Factor

Cell Rep Med

BACH2 promotes seeding and establishment of long-lived HIV-1 reservoir in memory CD4+ T cells. [Abstract]

2025 Aug 20:102311. PMID: 40845840
Phytomedicine

Wikstrol B reactivates latent human immunodeficiency virus (HIV-1) via the nuclear factor-κB (NF-κB) pathway. [Abstract]

2025 Jun:141:156667. PMID: 40233507
Phytomedicine

Sennoside A, derived from the traditional chinese medicine plant Rheum L., is a new dual HIV-1 inhibitor effective on HIV-1 replication. [Abstract]

2016 Nov 15;23(12):1383-1391. PMID: 27765358
Life Sci

Differential effects of dolutegravir, bictegravir and raltegravir in adipokines and inflammation markers on human adipocytes. [Abstract]

2022 Nov 1:308:120948. PMID: 36096241

Raltegravir purchased from MedChemExpress. Usage Cited in: Life Sci. 2022 Nov 1:308:120948. [Abstract]

Effects of dolutegravir, Raltegravir (0.1-10 μM) and bictegravir on adipogenic differentiation of SGBS human pre-adipocytes in culture. SGBS human pre-adipocytes were differentiated in culture in the presence of the indicated concentrations of drugs. Treatment was initiated on day 0 and continued throughout the differentiation process (10 days). Representative micrographs of adipocyte cell cultures differentiating in the presence of the indicated concentrations of drugs are shown.

Raltegravir purchased from MedChemExpress. Usage Cited in: Life Sci. 2022 Nov 1:308:120948. [Abstract]

Effects of dolutegravir (DTG), Raltegravir (RAL) (0.01-10 μM), and bictegravir (BIC) on the expression levels of inflammatory genes in differentiating SGBS human adipocytes. SGBS human pre-adipocytes were differentiated in culture in the presence of the indicated concentrations of drugs.

Raltegravir purchased from MedChemExpress. Usage Cited in: Life Sci. 2022 Nov 1:308:120948. [Abstract]

Effects of dolutegravir (DTG), Raltegravir (RAL) (0.1-10 μM), and bictegravir (BIC) on the release of leptin and adiponectin to the cell culture medium of differentiating SGBS human adipocytes. SGBS human pre-adipocytes were differentiated in culture in the presence of the indicated concentrations of drugs. Data corresponds to concentrations accumulating in the cell culture medium in the last 5 days of culture.
Pharmaceuticals (Basel)

HIV-1 Integrase Inhibition Activity by Spiroketals Derived from Plagius flosculosus, an Endemic Plant of Sardinia (Italy) and Corsica (France). [Abstract]

2023 Aug 8;16(8):1118. PMID: 37631033

Raltegravir purchased from MedChemExpress. Usage Cited in: Pharmaceuticals (Basel). 2023 Aug 8;16(8):1118. [Abstract]

Normalized antiviral activity of Raltegravir (48 h) as determined against NL4-3 HIV-1 wild-type strain in TZM-bl cell line. The nonlinear fitting curve as calculated by GraphPad Prism is depicted in red; the black lines indicate the dose-response curves. The R² of nonlinear fitting curve is 0.913 for Raltegravir.
Molecules

Privileged Scaffold Decoration for the Identification of the First Trisubstituted Triazine with Anti-SARS-CoV-2 Activity. [Abstract]

2022 Dec 12;27(24):8829. PMID: 36557962
J Infect Dis

Second-generation HIV integrase inhibitors induce differentiation dysregulation and exert toxic effects in human embryonic stem cell and mouse models. [Abstract]

2022 Nov 28;226(11):1992-2001. PMID: 36124861
J Mol Biol

Novel RNase H Inhibitors Blocking RNA-directed Strand Displacement DNA Synthesis by HIV-1 Reverse Transcriptase. [Abstract]

2022 Apr 15;434(7):167507. PMID: 35217069

Raltegravir purchased from MedChemExpress. Usage Cited in: J Mol Biol. 2022 Apr 15;434(7):167507. [Abstract]

HIV-1 integrase strand transfer inhibition assays. Bar graphs represent strand transfer activity inhibition in assays carried out with heteropolymeric hybrids in the presence of β-thujaplicinol, SL-6h, WX-II-25, II-4, XQ9, YLC2-155, DW3, K04-9 and K04-81, at 1 µM (purple), 5 µM (green), 10 µM (red) and 25 µM (blue), and Raltegravir (5 min) at 1 µM.
Virol Sin

Spastin is required for human immunodeficiency virus-1 efficient replication through cooperation with the endosomal sorting complex required for transport (ESCRT) protein. [Abstract]

2023 Jun;38(3):448-458. PMID: 37172824

Raltegravir purchased from MedChemExpress. Usage Cited in: Virol Sin. 2023 Jun;38(3):448-458. [Abstract]

VSV-G-pseudotyped HIV-1 virions were added and the inoculated cells were incubated for 24 h. Heat inactivated virus (H.I.) and integrase inhibitor Raltegravir (RAL, 30 nmol/L) were used as negative controls. After 24 h, the total cellular DNA was isolated from virus-infected cells. Integrated HIV-1 DNA was quantified by nested Alu-PCR. The numbers of infected cells and integrated HIV-1 DNA in siRNA-transfected cells were normalized to NC siRNA-transfected cells and reported as mean (±SEM) of three independent experiments.
Mol Divers

A potent and selective PROTAC degrader of CDK9 as effective inhibitor of HIV-1 RNA synthesis. [Abstract]

2025 Nov 12. PMID: 41225073

Raltegravir purchased from MedChemExpress. Usage Cited in: Mol Divers. 2025 Nov 12. [Abstract]

Raltegravir (anti-HIV-1 inhibitor). Integrated HIV-1 provirus DNA was determined by Alu-PCR. Results were normalized with that of the control group and are presented as fold reduction.
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
J Virol

Inhibition of Human Cytomegalovirus pUL89 Terminase Subunit Blocks Virus Replication and Genome Cleavage. [Abstract]

2017 Jan 18;91(3). pii: e02152-16. PMID: 27881652

Raltegravir purchased from MedChemExpress. Usage Cited in: J Virol. 2017 Jan 18;91(3). pii: e02152-16. [Abstract]

Inhibitory effects of Raltegravir on pUL89-C activity analyzed by agarose gel assay. Linearized pUC18 in the absence (Lane 1) or presence (Lane 2) of pUL89-C. Lanes 3–10: A range of concentrations of Raltegravir with pUL89-C. Numbers above bands correspond to the fold change compared with the control.
Viruses

Efficacy of Integrase Strand Transfer Inhibitors and the Capsid Inhibitor Lenacapavir against HIV-2, and Exploring the Effect of Raltegravir on the Activity of SARS-CoV-2. [Abstract]

2024 Oct 13;16(10):1607. PMID: 39459940
Viruses

Analysis and Molecular Determinants of HIV RNase H Cleavage Specificity at the PPT/U3 Junction. [Abstract]

2021 Jan 18;13(1):131. PMID: 33477685
J Neuroimmune Pharmacol

Combined Medication of Antiretroviral Drugs Tenofovir Disoproxil Fumarate, Emtricitabine, and Raltegravir Reduces Neural Progenitor Cell Proliferation In Vivo and In Vitro. [Abstract]

2017 Dec;12(4):682-692. PMID: 28735382

Raltegravir purchased from MedChemExpress. Usage Cited in: J Neuroimmune Pharmacol. 2017 Dec;12(4):682-692. [Abstract]

TDF/FTC/RAL combined medication induces mouse NPC apoptosis in vitro. Mouse NPCs are treated with either DMSO or TDF/FTC/RAL for 8 h. Cleaved Caspase-3 levels are determined by Western blotting.
Bioorg Med Chem

Design, synthesis and biological evaluation of 3-hydroxyquinazoline-2,4(1H,3H)-diones as dual inhibitors of HIV-1 reverse transcriptase-associated RNase H and integrase. [Abstract]

2019 Sep 1;27(17):3836-3845. PMID: 31324562
Clin Drug Investig

HIV Integrase Inhibitor Pharmacogenetics: An Exploratory Study. [Abstract]

2019 Mar;39(3):285-299. PMID: 30623371
PLoS One

Prenylated phloroglucinols from Hypericum scruglii, an endemic species of Sardinia (Italy), as new dual HIV-1 inhibitors effective on HIV-1 replication. [Abstract]

2018 Mar 30;13(3):e0195168. PMID: 29601601
Virology

Structure-based virtual screening of ROCK1 inhibitors for the discovery of Enterovirus-A71 antivirals. [Abstract]

2023 Aug:585:205-214. PMID: 37384967
Plant Biosyst

2018, 1-8.
SSRN

2026 Jun 23.
University of Debrecen

2023.
bioRxiv

Mechanistic insights and in vivo HIV suppression by the BRD4-targeting small molecule ZL0580. [Abstract]

2025 Aug 14:2025.08.14.670267. PMID: 40832229
Preprints

2024 Apr 23.
Preprints

2024 Feb 19.
SSRN

2023 Mar 30.
PeerJ Physical Chemistry

2019, 1:e6.

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (225.01 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

2.2501 mL

11.2506 mL

22.5012 mL

5 mM

0.4500 mL

2.2501 mL

4.5002 mL

10 mM

0.2250 mL

1.1251 mL

2.2501 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

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 3

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

Solubility: ≥ 2.5 mg/mL (5.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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

Protocol

Kinase Assay^[1]

For quantitative strand transfer assays, donor DNA substrate is formed by annealing HPLC grade oligonucleotides 5'-GACTCACTATAGGGCACGCGTCAAAATTCCATGACA and 5'-ATTGTCATG GAATTTTGACGCGTGCCCTATAGTGAGTC. Reactions (40 μL) contains 0.75 μM PFV IN, 0.75 μM donor DNA, 4 nM (300 ng) supercoiled pGEM9-Zf(−) target DNA, 125 mM NaCl, 5 mM MgSO₄, 4 μM ZnCl₂, 10 mM DTT, 0.8% (vol/vol) DMSO, and 25 mM BisTris propane-HCl, pH 7.45. Raltegravir is added at indicated concentrations. Reactions are initiated by addition of 2 μL PFV IN diluted in 150 mM NaCl, 2 mM DTT, and 10 mM Tris-HCl, pH 7.4, and stopped after 1 hour at 37°C by addition of 25 mM EDTA and 0.5% (wt/vol) SDS. Reaction products, deproteinized by digestion with 20 μg proteinase K for 30 minutes at 37°C followed by ethanol precipitation, are separated in 1.5% agarose gels and visualized by staining with ethidium bromide. Integration products are quantified by quantitative real-time PCR, using Platinum SYBR Green qPCR SuperMix and three primers: 5'-CTACTTACTCTAGCTTCCCGGCAAC, 5'-TTCGCCAGTTAATAGTTTGCGCAAC, and 5'-GACTCACTATAGGGCACGCGT. PCR reactions (20 μL) contained 0.5 μM of each primer and 1 μL diluted integration reaction product. Following a 5-min denaturation step at 95°C, 35 cycles are carried out in a CFX96 PCR instrument, using 10 seconds denaturation at 95°C, 30 seconds annealing at 56°C and 1 minutes extension at 68°C. Standard curves are generated using serial dilutions of WT PFV IN reaction in the absence of INSTI.

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

Cell Assay^[5]

Human MT-4 cells are infected for 2 hours with the SIVmac251, HIV-1 (IIIB) and HIV-2 (CDC 77618) stocks at a multiplicity of infection of, approximately, 0.1. Cells are then washed three times in phosphate buffered saline, and suspended at 5 × 10⁵/mL in fresh culture medium (to primary cells 50 units/mL of IL-2 are added) in 96-well plates, in the presence or absence of a range of triplicate raltegravir concentrations (0.0001 μM-1 μM). Untreated infected and mock-infected controls are prepared too, in order to allow comparison of the data derived from the different treatments. Viral cytopathogeniciy in MT-4 cells is quantitated by the methyl tetrazolium (MTT) method (MT-4/MTT assay) when extensive cell death in control virus-infected cell cultures is detectable microscopically as lack of capacity to re-cluster. The capability of MT-4 cells to form clusters after infection. Briefly, clusters are disrupted by pipetting; and, after 2 hours of incubation at 37°C, the formation of new clusters is assessed by light microscopy (100× magnification). Cell culture supernatants are collected for HIV-1 p24 and HIV-2/SIVmac251 p27 core antigen measurement by ELISA. In CEMx174-infected cell cultures, which show a propensity to form syncytia induced by the virus envelope glycoproteins, syncytia are counted, in blinded fashion, by light microscopy for each well at 5 days following infection.

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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)

References

[1]. Hare, S., et al., Molecular mechanisms of retroviral integrase inhibition and the evolution of viral resistance. Proc Natl Acad Sci U S A, 2010. 107(46): p. 20057-62. [Content Brief]

[2]. Xu P, et al. Combined Medication of Antiretroviral Drugs Tenofovir Disoproxil Fumarate, Emtricitabine, and Raltegravir Reduces Neural Progenitor Cell Proliferation In Vivo and In Vitro. J Neuroimmune Pharmacol. 2017 Dec;12(4):682-692. [Content Brief]

[3]. Hicks C, et al. Raltegravir: the first HIV type 1 integrase inhibitor. Clin Infect Dis. 2009 Apr 1;48(7):931-9 [Content Brief]

[4]. Moss DM, et al. Divalent metals and pH alter raltegravir disposition in vitro. Antimicrob Agents Chemother. 2012 Jun;56(6):3020-6 [Content Brief]

[5]. Hare S, et al. Structural and functional analyses of the second-generation integrase strand transfer inhibitor dolutegravir (S/GSK1349572). Mol Pharmacol. 2011 Oct;80(4):565-72. [Content Brief]

[6]. Lewis, M.G., et al. Response of a simian immunodeficiency virus (SIVmac251) to raltegravir: a basis for a new treatment for simian AIDS and an animal model for studying lentiviral persistence during antiretroviral therapy. Retrovirology, 2010. 7: p. 21. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2501 mL	11.2506 mL	22.5012 mL	56.2531 mL
	5 mM	0.4500 mL	2.2501 mL	4.5002 mL	11.2506 mL
	10 mM	0.2250 mL	1.1251 mL	2.2501 mL	5.6253 mL
	15 mM	0.1500 mL	0.7500 mL	1.5001 mL	3.7502 mL
	20 mM	0.1125 mL	0.5625 mL	1.1251 mL	2.8127 mL
	25 mM	0.0900 mL	0.4500 mL	0.9000 mL	2.2501 mL
	30 mM	0.0750 mL	0.3750 mL	0.7500 mL	1.8751 mL
	40 mM	0.0563 mL	0.2813 mL	0.5625 mL	1.4063 mL
	50 mM	0.0450 mL	0.2250 mL	0.4500 mL	1.1251 mL
	60 mM	0.0375 mL	0.1875 mL	0.3750 mL	0.9376 mL
	80 mM	0.0281 mL	0.1406 mL	0.2813 mL	0.7032 mL
	100 mM	0.0225 mL	0.1125 mL	0.2250 mL	0.5625 mL

Keywords

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Raltegravir

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

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Rare Diseases Drug Library

Pediatric Drug Library

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Non-steroidal Anti-Inflammatory Compound Library

Off-patent Drug Library

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MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

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FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Raltegravir

All HIV Isoforms

Biological Activity

Chemical Information

Publications (27)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Raltegravir

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

Targeted Diversity Library

Rare Diseases Drug Library

Pediatric Drug Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Non-steroidal Anti-Inflammatory Compound Library

Off-patent Drug Library

Metabolic Enzyme 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

Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Raltegravir

All HIV Isoforms

Biological Activity

Chemical Information

Publications (27)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Raltegravir Related Classifications

Cat. No.: HY-10353