MK-2048

• UNSPSC Description:

  MK-2048 is a potent inhibitor of integrase and INR263K with IC50 of 2.6 nM and 1.5 nM, respectively. IC50 Value: 2.6 nM for HIV Integrase Target: HIV Integrase MK-2048 is a second generation integrase inhibitor, intended to be used against HIV infection. MK-2048 inhibits subtype B and subtype C integrase activities. MK-2048 inhibits R263K mutants slightly more effectively than G118R mutants. MK-2048 inhibits S217H intasome and, by contrast, MK-2048 remains fully active against the N224H intasome. MK-2048 displays substantially lower dissociation rates compared with raltegravir, another integrase inhibitor. MK-2048 is active against viruses resistant to RAL and EVG. MK-2048 exposure leads to the selection of G118R as a possible novel resistance mutation after 19 weeks. MK-2048, with continued pressure, subsequently leads to an additional substitution, at position E138K, after 29 weeks, within the IN gene. Although the G118R mutation alone confers only slight resistance to MK-2048 but not to RAL or EVG, its presence arouses a dramatic reduction in viral replication capacity compared to wild-type NL4-3. E138K both partially restores viral replication capacity and also contributes to increased levels of resistance against MK-2048.

• Target Antigen:

  HIV; HIV Integrase

• Type:

  Reference compound

• Related Pathways:

  Anti-infection;Metabolic Enzyme/Protease

• Applications:

  COVID-19-anti-virus

• Field of Research:

  Infection

• Assay Protocol:

  https://www.medchemexpress.com/mk-2048.html

• Purity:

  98.0

• Solubility:

  10 mM in DMSO

• Smiles:

  FC1=C(Cl)C=C(CN2C(C(C(O)=C3N4[C@@H](C)CN(CC)C3=O)=C4C(C(NC)=O)=N2)=O)C=C1

• Molecular Weight:

  461.87

• References & Citations:

  [1]L. Van Wesenbeeck, E. Rondelez, M. Feyaerts, et al. Cross-Resistance Profile Determination of Two Second-Generation HIV-1 Integrase Inhibitors Using a Panel of Recombinant Viruses Derived from Raltegravir-Treated Clinical Isolates .Antimicrob. Agents Chemother. 2011, 55 (1): 321-325|[2]Muhammad Esa Seegulam, Lee Ratner. Integrase Inhibitors Effective against Human T-Cell Leukemia Virus Type 1. Antimicrob. Agents Chemother. 2011, 55 (5): 2011-2017|[3]Tamara Bar-Magen1, Richard D. Sloan1, Daniel A. Donahue1, et al. Identification of Novel Mutations Responsible for Resistance to MK-2048, a Second-Generation HIV-1 Integrase Inhibitor. J. Virol. 2010, 84(18): 9210-9216|[4]Laith Q Al-Mawsawi, Rasha I Al-Safi, Nouri Neamati. Anti-infectives Clinical progress of HIV-1 integrase inhibitors. 2008, 13(2): Pages 213-225|[5]Al-Mawsawi LQ, Al-Safi RI, Neamati N. Anti-infectives: clinical progress of HIV-1 integrase inhibitors. Expert Opin Emerg Drugs. 2008 Jun;13(2):213-25.

• Shipping Conditions:

  Blue Ice

• Storage Conditions:

  -20°C, 3 years (Powder)

• Clinical Information:

  Phase 1

• CAS Number:

  869901-69-9