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

Raltegravir potassium salt (Synonyms: MK 0518 potassium salt)

Cat. No.: HY-10353A Purity: 99.65%
Handling Instructions

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

For research use only. We do not sell to patients.
Raltegravir potassium salt Chemical Structure

Raltegravir potassium salt Chemical Structure

CAS No. : 871038-72-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 92 In-stock
5 mg USD 84 In-stock
10 mg USD 144 In-stock
50 mg USD 468 In-stock
100 mg USD 720 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of Raltegravir potassium salt:

    Raltegravir potassium salt purchased from MCE. Usage Cited in: J Virol. 2016 Nov 23. pii: JVI.02152-16.

    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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Raltegravir (potassium salt) is a potent 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 IC95 of 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].

    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].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.0725 mL 10.3625 mL 20.7250 mL
    5 mM 0.4145 mL 2.0725 mL 4.1450 mL
    10 mM 0.2072 mL 1.0362 mL 2.0725 mL
    Please refer to the solubility information to select the appropriate solvent.
    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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    482.51

    Formula

    C₂₀H₂₀FKN₆O₅

    CAS No.

    871038-72-1

    SMILES

    O=C(C(N=C(C(NC(C1=NN=C(C)O1)=O)(C)C)N2C)=C([O-])C2=O)NCC3=CC=C(F)C=C3.[K+]

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Product Name:
    Raltegravir potassium salt
    Cat. No.:
    HY-10353A
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