MK-2048 - 10mM in DMSO , CAS No.869901-69-9

CAS: 869901-69-9 Cat. No.: M408622 Formula: C₂₁H₂₁ClFN₅O₄ Peso molecolare: 461.87

GRADE & PURITY 10mM in DMSO

Synonyms

Pyrazino[1',2':1,5]pyrrolo[2,3-d]pyridazine-4-carboxamide, 2-[(3-chloro-4-fluorophenyl)methyl]-8-ethyl-1,2,6,7,8,9-hexahydro-10-hydroxy-N,6-dimethyl-1,9-dioxo-, (6S)-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

Information

MK-2048 MK-2048 is a potent inhibitor of integrase (IN) and IN R263K with IC50 of 2.6 nM and 1.5 nM, respectively.
In vitro

MK-2048 inhibits subtype B and subtype C integrase activities with IC50 of 75 nM and 80 nM, respectively. Disintegration is prevented by high concentrations of MK-2048 to a comparable extent with both subtype B and C enzymes. Mutation at the site of R263K slightly increases integrase susceptibility to MK-2048. G118R translates into a decrease in integrase activity and confers resistance to MK-2048. MK-2048 inhibits S217H intasome with an IC50 of 900 nM. By contrast, MK2048 remains fully active against the N224H intasome with an IC50 of 25 nM. MK2048 displays substantially lower dissociation rates compared with raltegravir, another integrase inhibitor. The subsequent selection of E138K partially restores replication capacity to approximately 13% of wt levels and increased resistance to MK-2048 to approximately 8-fold. MK-2048 is active against viruses resistant to RAL and EVG. Exposure to MK-2048 leads to the selection of G118R as a possible novel resistance mutation after 19 weeks. Continued pressure with MK-2048 subsequently leads to an additional substitution after 29 weeks at position E138K, 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.

In vivo

Cell Data

cell lines：

Concentrations：0.0256 nM to 2 μM

Incubation Time：72 hours

Powder Purity:≥99%

Specifications

Sinonimi

Pyrazino[1',2':1,5]pyrrolo[2,3-d]pyridazine-4-carboxamide, 2-[(3-chloro-4-fluorophenyl)methyl]-8-ethyl-1,2,6,7,8,9-hexahydro-10-hydroxy-N,6-dimethyl-1,9-dioxo-, (6S)-

Specifiche e purezza

10mM in DMSO

Meccanismi biochimici e fisiologici

MK-2048 is a potent inhibitor of integrase (IN) and IN_R263K with IC50 of 2.6 nM and 1.5 nM, respectively.

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Nomi e identificatori

• Isomeri SMILES: CCN1C[C@@H](N2C3=C(C(=C2C1=O)O)C(=O)N(N=C3C(=O)NC)CC4=CC(=C(C=C4)F)Cl)C
• Peso molecolare: 461.87
• Reaxy-Rn: 22829520
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=22829520&ln=

Domande frequenti

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 869901-69-9, the molecular formula is C21H21ClFN5O4, and the molecular weight is 461.87 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.