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MK 0518, MK-0518, MK0518, N-[(4-Fluorophenyl)methyl]-1,6-dihydro-5-hydroxy-1-methyl-2-[1-methyl-1-[[(5-methyl-1,3,4-oxadiazol-2-yl)carbonyl]amino]ethyl]-6-oxo-4-pyrimidinecarboxamide
C20H21FN6O5
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Quality Level
Assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Biochem/physiol Actions
Raltegravir (MK-0518) is an orally active, potent and selective HIV type-1 (HIV-1) integrase inhibitor (IC50 = 2-7 nM; ineffctive against HIV-1 reverse transcriptase or protease) that prevents HIV-1 cellular replication by blocking viral cDNA integration into host genome in cultures (IC50 = 19 nM & 33 nM in the presence of 10% fetal bovine serum or 50% human serum) and in vivo.
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
新产品
Certificates of Analysis (COA)
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Drugs, 68(1), 131-138 (2007-12-18)
* Raltegravir, the first in a new class of orally administered HIV type-1 (HIV-1) integrase inhibitors, selectively inhibits the strand transfer activity of HIV-1 and its integration into human DNA, a key stage in retroviral propagation, thereby limiting viral replication
Antiretroviral activity, pharmacokinetics, and tolerability of MK-0518, a novel inhibitor of HIV-1 integrase, dosed as monotherapy for 10 days in treatment-naive HIV-1-infected individuals
Journal of Acquired Immune Deficiency Syndromes, 43(5), 509-515 (2006)
Life sciences, 308, 120948-120948 (2022-09-13)
To assess the potential direct effects of the integrase strand-transfer inhibitors (INsTIs) dolutegravir, bictegravir, and raltegravir, drugs used as treatment for people living with human immunodeficiency virus (PLWH), on human adipose cells. Drugs were added to the differentiation medium of
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