Raltegravir

SKU: orb1305950

Description

Raltegravir

Research Area

Infectious Disease & Virology, Protein Biochemistry

Key Properties

• CAS Number: 518048-05-0
• MW: 444.42
• Purity: 99.86%
• Formula: C₂₀H₂₁FN₆O₅
• SMILES: Cc1nnc(o1)C(=O)NC(C)(C)c1nc(C(=O)NCc2ccc(F)cc2)c(O)c(=O)n1C
• Target: Integrase,HIV Protease
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:250 mg/mL (562.53 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (11.25 mM)

Bioactivity

• Target IC50:
  Integrase (S217Q PFV):40 nM|Integrase (WT PFV):90 nM
• In Vivo:
  Raltegravir effectively inhibits HIV-1 in vitro with a 95% inhibitory concentration of 31±20 nM in human T lymphocyte cultures. It maintains similar sensitivity to the S217Q PFV IN mutation as compared to the wild-type enzyme. In the human lymphoid CD4+ T cell lines MT-4 and CEMx174, raltegravir potently suppresses SIVmac251 replication, demonstrating an EC90 in the low nanomolar range. It weakly inhibits cytochrome P450 liver enzymes and does not induce the expression of CYP3A4 RNA or the activity of the CYP3A4-dependent 6-β-hydroxylase enzyme involved in testosterone metabolism. The presence of magnesium and calcium reduces raltegravir's cell permeability. Raltegravir, along with related HIV-1 integrase strand transfer inhibitors, effectively blocks viral replication.
• In Vitro:
  Raltegravir induces immunological improvement in non-human primate viruses, accompanied by progressive SIVmac251 infection.
• Cell Research:
  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. (Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Raltegravir, HIV, HIV Protease, HIV Integrase, HIVProtease, Human immunodeficiency virus, Integrase (S217Q PFV), Integrase (WT PFV), Inhibitor, MK0518, MK-0518, MK 0518, inhibit

Compound Identifiers

PubChem CID

54671008