1. Metabolic Enzyme/Protease
    Anti-infection
  2. HIV Integrase
    HIV
  3. Raltegravir sodium

Raltegravir sodium (Synonyms: MK 0518 sodium)

Cat. No.: HY-10353B
Handling Instructions

Raltegravir (MK 0518) sodium is a potent and orally active integrase (IN) inhibitor, used to treat HIV infection.

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

Raltegravir sodium Chemical Structure

Raltegravir sodium Chemical Structure

CAS No. : 1292804-07-9

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Other In-stock Forms of Raltegravir sodium:

Other Forms of Raltegravir sodium:

Top Publications Citing Use of Products

    Raltegravir sodium purchased from MCE. Usage Cited in: J Virol. 2017 Jan 18;91(3). pii: e02152-16.

    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.

    Raltegravir sodium purchased from MCE. Usage Cited in: J Neuroimmune Pharmacol. 2017 Dec;12(4):682-692.

    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.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Raltegravir (MK 0518) sodium is a potent and orally active integrase (IN) inhibitor, used to treat HIV infection.

    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].

    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].

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

    Molecular Weight

    466.40

    Formula

    C20H20FN6NaO5

    CAS No.
    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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

     

    Salutation

    Applicant Name *

     

    Email address *

    Phone number *

     

    Organization name *

    Department *

     

    Requested quantity *

    Country or Region *

         

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Raltegravir sodium
    Cat. No.:
    HY-10353B
    Quantity:
    MCE Japan Authorized Agent: