Raltegravir sodium
Based on 28 publication(s) in Google Scholar
Raltegravir (MK 0518) sodium is a potent and orally active integrase (IN) inhibitor, used to treat HIV infection.
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- CAS No.: 1292804-07-9
- Formule: C20H20FN6NaO5
- Masse moléculaire:466.40
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Publications Citing Use of MedChemExpress (MCE) Raltegravir sodium
More- Cell Rep Med. 2025 Aug 20:102311. [Abstract]
- Phytomedicine. 2025 Jun:141:156667. [Abstract]
- Phytomedicine. 2016 Nov 15;23(12):1383-1391. [Abstract]
- Life Sci. 2022 Nov 1:308:120948. [Abstract]
- J Neuroimmune Pharmacol. 2017 Dec;12(4):682-692. [Abstract]
- Pharmaceuticals (Basel). 2023 Aug 8;16(8):1118. [Abstract]
- Molecules. 2022 Dec 12;27(24):8829. [Abstract]
- Virol Sin. 2023 Jun;38(3):448-458. [Abstract]
- J Mol Biol. 2022 Apr 15;434(7):167507. [Abstract]
- Mol Divers. 2025 Nov 12. [Abstract]
- J Infect Dis. 2022 Nov 28;226(11):1992-2001. [Abstract]
- J Virol. 2017 Jan 18;91(3):e02152-16. [Abstract]
- Open Forum Infect Dis. 2024 Nov 29;12(1):ofae705. [Abstract]
- Viruses. 2024 Oct 13;16(10):1607. [Abstract]
- Viruses. 2021 Jan 18;13(1):131. [Abstract]
- Bioorg Med Chem. 2019 Sep 1;27(17):3836-3845. [Abstract]
- Clin Drug Investig. 2019 Mar;39(3):285-299. [Abstract]
- PLoS One. 2018 Mar 30;13(3):e0195168. [Abstract]
- Virology. 2026 Jun 4:623:110991. [Abstract]
- Virology. 2023 Aug:585:205-214. [Abstract]
- Plant Biosyst. 2018, 1-8.
- SSRN. 2026 Jun 23.
- University of Debrecen. 2023.
- bioRxiv. 2025 Aug 14:2025.08.14.670267. [Abstract]
- Preprints. 2024 Apr 23.
- Preprints. 2024 Feb 19.
- SSRN. 2023 Mar 30.
- PeerJ Physical Chemistry. 2019, 1:e6.
Customer Validation & Images
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RT-PCR
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Cell Proliferation/Viability Assay
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RT-PCR
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Cell Proliferation/Viability Assay
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RT-PCR
Activité biologique
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HIV-1 |
HIV-2 |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1292804-07-9
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Masse moléculaire 466.40
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Formule C20H20FN6NaO5
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SMILES
O=C(C(N=C(C(NC(C1=NN=C(C)O1)=O)(C)C)N2C)=C(O[Na])C2=O)NCC3=CC=C(F)C=C3
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Synonyms
MK 0518 sodium
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (28)
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Journal Impact Factor
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Most Recent
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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 sodium 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 sodium 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 sodium 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.
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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 sodium 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.
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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 sodium 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.
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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 -
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 sodium 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.
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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 sodium 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.
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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 sodium 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.
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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 Virol
Inhibition of Human Cytomegalovirus pUL89 Terminase Subunit Blocks Virus Replication and Genome Cleavage. [Abstract]2017 Jan 18;91(3):e02152-16. PMID: 27881652
Raltegravir sodium purchased from MedChemExpress. Usage Cited in: J Virol. 2017 Jan 18;91(3):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.
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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 -
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 -
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
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
Generation and evaluation of an EcoHIV mouse model to study HIV-1 integration and expression. [Abstract]2026 Jun 4:623:110991. PMID: 42320113 -
Virology
Structure-based virtual screening of ROCK1 inhibitors for the discovery of Enterovirus-A71 antivirals. [Abstract]2023 Aug:585:205-214. PMID: 37384967 -
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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 -
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Pureté et documentation
Références
[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]
Calculators
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Raltegravir sodium Related Classifications
HY-10353B Related Classifications
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