MK-5172 (Synonyms: MK-5172) |
Catalog No.GC18004
One-Click Copy Product Info
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MK-5172 is a selective inhibitor of hepatitis C virus (HCV) NS3/4a protease, exhibiting broad-spectrum activity against multiple genotypes and drug-resistant variants, and capable of inhibiting SARS-CoV-2 3CL protease activity.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1350514-68-9
Sample solution is provided at 25 µL, 10mM.
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MK-5172 is a selective inhibitor of hepatitis C virus (HCV) NS3/4a protease, exhibiting broad-spectrum activity against multiple genotypes and drug-resistant variants, and capable of inhibiting SARS-CoV-2 3CL protease activity[1-2]. MK-5172 demonstrates favorable liver-targeting properties and sustained virological responses in studies, making MK-5172 applicable for research related to chronic hepatitis C and MK-5172 co-infection with HIV[3-4].
In vitro, pretreatment of Vero E6 cells or human-derived 293T-ACE2 cells with MK-5172 (0.55-20.5μM) for 2 hours, followed by infection with SARS-CoV-2 virus (MOI=0.025–2PFU/cell) for 48 hours, significantly inhibited viral replication[5]. Treatment of GT1a (H77) replicon cells with MK-5172 (0.4–35nM) for 72 hours, MK-5172 significantly suppressed HCV RNA replication (EC₉₀=0.9nM) and maintained inhibitory activity against NS5A-resistant variants[6].
In vivo, intraperitoneal injection of MK-5172 (10mg/kg/day) for 5 days (starting from day 5 after MC-38 colon adenocarcinoma cell transplantation) in PD-1-mCherry-SMASh homozygous knock-in (KI) mice significantly suppressed tumor growth[7]. Oral administration of MK-5172 (3mg/kg) once daily for 3 consecutive days in diabetic model C57BL/6 mice significantly restored glucose homeostasis[8].
References:
[1] Vallet-Pichard A, Pol S. Grazoprevir/elbasvir combination therapy for HCV infection. Therap Adv Gastroenterol. 2017 Jan;10(1):155-167.
[2] Al-Salama ZT, Deeks ED. Elbasvir/Grazoprevir: A Review in Chronic HCV Genotypes 1 and 4. Drugs. 2017 May;77(8):911-921.
[3] Karaoui LR, Mansour H, Chahine EB. Elbasvir-grazoprevir: A new direct-acting antiviral combination for hepatitis C. Am J Health Syst Pharm. 2017 Oct 1;74(19):1533-1540.
[4] Wang SJ, Huang CF, Yu ML. Elbasvir and grazoprevir for the treatment of hepatitis C. Expert Rev Anti Infect Ther. 2021 Sep;19(9):1071-1081.
[5] Bafna K, White K, Harish B, et al. Hepatitis C virus drugs that inhibit SARS-CoV-2 papain-like protease synergize with remdesivir to suppress viral replication in cell culture. Cell Rep. 2021 May 18;35(7):109133.
[6] Lahser FC, Bystol K, Curry S, et al. The Combination of Grazoprevir, a Hepatitis C Virus (HCV) NS3/4A Protease Inhibitor, and Elbasvir, an HCV NS5A Inhibitor, Demonstrates a High Genetic Barrier to Resistance in HCV Genotype 1a Replicons. Antimicrob Agents Chemother. 2016 Apr 22;60(5):2954-64.
[7] Naruse C, Sugihara K, Miyazaki T, et al. A degron system targeting endogenous PD-1 inhibits the growth of tumor cells in mice. NAR Cancer. 2022 Jun 17;4(2):zcac019.
[8] Shao J, Li S, Qiu X, et al. Engineered poly(A)-surrogates for translational regulation and therapeutic biocomputation in mammalian cells. Cell Res. 2024 Jan;34(1):31-46.
| Cell experiment [1]: | |
Cell lines | Vero E6 cells (African green monkey kidney epithelial cell line) and human 293T cells expressing ACE2 |
Preparation Method | Vero E6 and 293T-ACE2 cells were maintained in Dulbecco's minimal essential medium (DMEM) supplemented with 10% fetal bovine serum (FBS). Cells were treated with MK-5172 (0.55-20.5μM) for 48 hours. |
Reaction Conditions | 4.2µM (in Vero E6 cells); 0.55-20.5µM range (in 293T-ACE2 cells); 48h. |
Applications | MK-5172 significantly inhibited SARS-CoV-2 replication in both Vero E6 (IC₅₀=4.2µM) and human 293T-ACE2 cells. MK-5172 demonstrated synergistic antiviral activity with remdesivir, increasing the efficacy of the polymerase inhibitor by up to 10-fold. The drug specifically inhibited the viral papain-like protease (PLpro) enzyme activity. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | Diabetic mice were generated by Streptozotocin (STZ) injection. Mice received daily oral administration of MK-5172 for 3 consecutive days. Blood glucose and insulin levels were measured, and intraperitoneal glucose tolerance tests (GTTs) were performed. |
Dosage form | 3mg/kg; Oral gavage; Once daily for 3 days |
Applications | MK-5172 administration effectively restored glucose homeostasis in diabetic mice, significantly reducing fasting blood glucose levels and improving glucose tolerance. The drug triggered insulin expression from a genetically encoded MK-5172-inducible translational switch, demonstrating therapeutic efficacy in a disease model requiring on-demand drug secretion. |
References: | |
| Cas No. | 1350514-68-9 | SDF | |
| Synonyms | MK-5172 | ||
| Canonical SMILES | COC1=CC2=C(N=C(CCCCC[C@@H]3C[C@H]3OC(N[C@@H](C(C)(C)C)C(N4[C@H](C(N[C@@]5(C(NS(=O)(C6CC6)=O)=O)[C@H](C5)C=C)=O)C[C@@H]7C4)=O)=O)C(O7)=N2)C=C1 | ||
| Formula | C38H50N6O9S | M.Wt | 766.9 |
| Solubility | ≥ 38.35 mg/mL in DMSO, ≥ 24 mg/mL in EtOH with ultrasonic and warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.304 mL | 6.5198 mL | 13.0395 mL |
| 5 mM | 260.8 μL | 1.304 mL | 2.6079 mL |
| 10 mM | 130.4 μL | 652 μL | 1.304 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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.)
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 saline, 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)