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MK-2048 Integrase inhibitor

Name: MK-2048
Brand: Selleck Chemicals
SKU: S2765
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S2765

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

Chemical Structure

Molecular Weight: 461.87

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S276501 DMSO]9 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.01%

99.01

Related Targets	Bacterial Antibiotics Anti-infection Fungal Antiviral COVID-19 Parasite Reverse Transcriptase HIV HCV Protease SARS-CoV HIV Protease Influenza Virus β-lactamase HBV CMV Neuraminidase HCV HSV RSV Enterovirus Thioredoxin Reductase 3C-Like Protease Ribosomal Peptidyl Transferase HPV
Related Products	BMS-707035 Robinetin Lavendustin B

Chemical Information, Storage & Stability

Molecular Weight	461.87	Formula	C₂₁H₂₁ClFN₅O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	869901-69-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCN1CC(N2C3=C(C(=C2C1=O)O)C(=O)N(N=C3C(=O)NC)CC4=CC(=C(C=C4)F)Cl)C

Solubility

In vitro
Batch:

DMSO : 9 mg/mL (19.48 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.45mg/ml (0.97mM)	Taking the 1 mL working solution as an example, add 50 μL of 9 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Integrase (R263K) ^[1] 1.5 nM Integrase ^[1] 2.6 nM
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 this compound to a comparable extent with both subtype B and C enzymes. Mutation at the site of R263K slightly increases integrase susceptibility to this inhibitor. G118R translates into a decrease in integrase activity and confers resistance to this chemical. ^[2] This compound inhibits S217H intasome with an IC50 of 900 nM. By contrast, it remains fully active against the N224H intasome with an IC50 of 25 nM. It displays substantially lower dissociation rates compared with raltegravir, another integrase inhibitor. ^[3] The subsequent selection of E138K partially restores replication capacity to approximately 13% of wt levels and increased resistance to this agent to approximately 8-fold. It is active against viruses resistant to RAL and EVG. Exposure to this compound leads to the selection of G118R as a possible novel resistance mutation after 19 weeks. Continued pressure with it 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 this inhibitor 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 this chemical. ^[4]
References	[1] https://pubmed.ncbi.nlm.nih.gov/22205735/ [2] https://pubmed.ncbi.nlm.nih.gov/19906306/ [3] https://pubmed.ncbi.nlm.nih.gov/21030679/ [4] https://pubmed.ncbi.nlm.nih.gov/20610719/

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