MK-2048

MK-2048 是一种有效的整合酶和 INR263K 抑制剂，IC50 分别为 2.6 nM 和 1.5 nM。

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库存: 现货

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数量
5mg

￥1600.00

1280.00

- +
10mg

￥2150.00

1720.00

- +
50mg

￥6212.00

4970.00

- +
100mg

￥9137.00

7310.00

- +

已选 0 种 0 瓶

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货号: ajci15364
CAS: 869901-69-9
别名:
分子式: C21H21ClFN5O4
分子量: 461.9
纯度: >98%
溶解度: ≥ 10.55 mg/mL in DMSO, ≥ 3.68 mg/mL in EtOH with ultrasonic and warming
储存: Store at -20°C
库存: 现货

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.
参考文献:
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.