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Merck
CN

SML3670

Raltegravir

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

别名:

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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关于此项目

经验公式(希尔记法):
C20H21FN6O5
化学文摘社编号:
分子量:
444.42
UNSPSC Code:
51111800
NACRES:
NA.25
MDL number:
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产品名称

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

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.

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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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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