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MK-2048

In stock
Catalog No.
A4072
Integrase inhibitor for HIV-1,second generation
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$350.00
In stock
5mg
$190.00
In stock
10mg
$260.00
In stock
50mg
$680.00
In stock
100mg
$980.00
In stock

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Email: [email protected]

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Background

MK-2048 is a second generation inhibitor of HIV-1 integrase with IC50 values of 0.075 μM and 0.08 μM for subtype B and subtype C integrase, respectively.
Integration of viral cDNA into the host genome is one of the definitive features of retrovirus replication. Integrase inhibitors are active against both B and non-B subtypes in therapy. Subtype C variants are responsible for approximately 50% of infections worldwide, mostly in Sub-Saharan Africa and India. After viral entry and reverse transcription, reverse-transcribed double-stranded blunt-ended DNA is incorporated into the host cell genome through two catalytic activities mediated by integrase. MK-2048 could inhibit the strand transfer process catalyzed by integrase.
The inhibition activity of MK-2048 against integrase was evaluated by means of purified recombinant subtype B and C integrase enzymes, which were obtained and amplified from viruses in long-term infected patients. Purified recombinant subtype B and C integrase enzymes were incubated with increasing concentrations of MK-2048 and corresponding templates. MK-2048 possesses inhibition activities for strand transfer against subtype B and C enzymes, whose IC50 values were 0.075 μM and 0.08 μM, respectively. Disintegration was inhibited by high concentrations of MK-2048 to a comparable extent with both subtype B and C enzymes.
Inhibition of replication by MK-2048 was also evaluated in cell culture based assays using cord blood mononuclear cells. EC50 for subtype B viruses varies from 0.0003 μM to 0.0148 μM and 0.0007 μM to 0.0033 μM for subtype C viruses.
References:
1.Bar-Magen T, Sloan R D, Faltenbacher V H, et al. Comparative biochemical analysis of HIV-1 subtype B and C integrase enzymes[J]. Retrovirology, 2009, 6(1): 103.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt461.9
Cas No.869901-69-9
FormulaC21H21ClFN5O4
Solubility≥10.55 mg/mL in DMSO, ≥3.68 mg/mL in EtOH with ultrasonic and warming, <2.2 mg/mL in H2O
Chemical Name(6S)-2-[(3-chloro-4-fluorophenyl)methyl]-8-ethyl-10-hydroxy-N,6-dimethyl-1,9-dioxo-6,7-dihydropyrazino[5,6]pyrrolo[1,3-b]pyridazine-4-carboxamide
SDFDownload SDF
Canonical SMILESCCN1CC(N2C3=C(C(=C2C1=O)O)C(=O)N(N=C3C(=O)NC)CC4=CC(=C(C=C4)F)Cl)C
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description MK-2048 is a second generation inhibitor of HIV-1 integrase with IC50 values of 0.075 μM and 0.08 μM for subtype B and subtype C integrase, respectively.
Targets subtype B integrase subtype C integrase        
IC50 0.075 μM 0.08 μM        

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