MK-2048
Product Sizes
5 mg
HY-13305-5MG
About this Product
- SKU:
- HY-13305
- CAS Number:
- 869901-69-9
- Extra Details:
- 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.
- Molecular Weight:
- 461.87
- Purity:
- 99.01
- References:
- [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.
- Research Area:
- Infection
- Shipping Conditions:
- Blue Ice
- Storage Conditions:
- -20[o]C; 3 years (Powder)
- Type:
- Proteins, Peptides, Small Molecules & Other Biomolecules: Small Molecules
- Pathway:
- Anti-infection;Metabolic Enzyme/Protease
