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SML3670

Sigma-Aldrich

Raltegravir

≥98% (HPLC)

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Synonym(s):
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
Empirical Formula (Hill Notation):
C20H21FN6O5
CAS Number:
Molecular Weight:
444.42
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.25

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

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Jamie D Croxtall et al.
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)
Pere Domingo et al.
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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