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Merck
CN

SML3670

Raltegravir

≥98% (HPLC), HIV-1 integrase inhibitor , powder

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

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About This Item

Empirical Formula (Hill Notation):
C20H21FN6O5
CAS Number:
518048-05-0
Molecular Weight:
444.42
UNSPSC Code:
51111800
NACRES:
NA.25
MDL number:
MFCD10698872

Key Documents

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Product Name

Raltegravir, ≥98% (HPLC)

SMILES string

Fc1ccc(cc1)CNC(=O)C2N=C(N(C(=O)C2=O)C)C(NC(=O)c3nnc([o]3)C)(C)C

InChI

1S/C20H21FN6O5/c1-10-25-26-17(32-10)16(30)24-20(2,3)19-23-13(14(28)18(31)27(19)4)15(29)22-9-11-5-7-12(21)8-6-11/h5-8,13H,9H2,1-4H3,(H,22,29)(H,24,30)

InChI key

DDGPCENTWMZXFO-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Quality Level

100

Related Categories

Biochem/physiol Actions

Orally active, potent and selective HIV type-1 (HIV-1) integrase inhibitor in cultures and in vivo.
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.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000456064
0000456064
0000447649
0000447652
0000447652

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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)
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
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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