Grazoprevir

Catalog No.S3728 Synonyms: MK5172

For research use only.

Grazoprevir anhydrous (MK5172) is a Hepatitis C Virus NS3/4A Protease inhibitor with IC50 values of 7pM, 4pM, and 62pM for HCV genotype 1a, 1B, and 4 respectively.

Grazoprevir Chemical Structure

CAS No. 1350514-68-9

Selleck's Grazoprevir has been cited by 5 Publications

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Biological Activity

Description Grazoprevir anhydrous (MK5172) is a Hepatitis C Virus NS3/4A Protease inhibitor with IC50 values of 7pM, 4pM, and 62pM for HCV genotype 1a, 1B, and 4 respectively.
Targets
gt1b [1]
(Cell-free assay)
gt1a [1]
(Cell-free assay)
gt1b R155K [1]
(Cell-free assay)
gt2a [1]
(Cell-free assay)
gt1b D168V [1]
(Cell-free assay)
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0.01 nM(Ki) 0.01 nM(Ki) 0.07 nM(Ki) 0.08 nM(Ki) 0.14 nM(Ki)
In vitro

MK-5172 is a novel P2-P4 quinoxaline macrocyclic NS3/4a protease inhibitor currently in clinical development. The compound demonstrates subnanomolar activity against a broad enzyme panel encompassing major hepatitis C virus (HCV) genotypes as well as variants resistant to earlier protease inhibitors[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HuH7 NHL3cnhCdnSrdnnyZYwh[XO|YYm= NIj3W3M4OiCqcoO= Mnm5RY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGNXKGenbn;0fZBmKDGjIHnu[oVkfGWmIHnuJIh2dWGwIFj1TFch[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjD2bZJidCC{ZYDsbYNifGmxbjDh[pRmeiB5MjDodpMh[nliUmStVGNTKG2ndHjv[EwhTUN3ME2wMlAxODQQvF2u NWe0WYpHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4NVk3PzZpPkK2PFE6Pjd4PD;hQi=>
HuH7 M3Lmb2FvfGm4aYLhcEBie3OjeR?= MmPVO|IhcHK| MnPORY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGNXKGenbn;0fZBmKDGkIHnu[oVkfGWmIHnuJIh2dWGwIFj1TFch[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjD2bZJidCC{ZYDsbYNifGmxbjDh[pRmeiB5MjDodpMh[nliUmStVGNTKG2ndHjv[EwhTUN3ME2wMlAxODQQvF2u NYPJXHdSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4NVk3PzZpPkK2PFE6Pjd4PD;hQi=>
HuH7 NVzZOFJGSW62aY\pdoFtKGG|c3H5 M1XZeVczKGi{cx?= NY\UeXN3SW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEOYIHflco91gXCnIEHhJIlv\mWldHXkJIlvKGi3bXHuJGh2UDdiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wII\pdoFtKFKQQTDs[ZZmdCCjZoTldkA4OiCqcoOgZpkhWlRvUFPSJI1mfGixZDygSWM2OD1yLkCwNFbPxE1w M1nEUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUm0O|U6Lz5{N{m5OFc2QTxxYU6=
HuH7 NXntOYN7SW62aY\pdoFtKGG|c3H5 NULQUWl1PzJiaILz MVnBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDIR3Yh\2Wwb4T5dIUhOWJiaX7m[YN1\WRiaX6gbJVu[W5iSIXIO{Bk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hfmm{YXygVm5CKGyndnXsJIFnfGW{IEeyJIhzeyCkeTDSWE1RS1JibXX0bI9lNCCHQ{WwQVAvODByNt88UU4> MnXzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3OVkoRjJ5OUm0O|U6RC:jPh?=
HuH7 NE[weFVCdnSrdnnyZYwh[XO|YYm= MkK1O|IhcHK| NXrZT|VESW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEOYIHflco91gXCnIELhJIlv\mWldHXkJIlvKGi3bXHuJGh2UDdiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB3cXKjbDDy[ZBtcWOjdHnvckBi\nSncjC3NkBpenNiYomgVnQuWEOUIH3leIhw\CxiRVO1NF0xNjByMUNOwG0v NIPQRno9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkixPVY4Pid-Mk[4NVk3PzZ:L3G+
HuH7 NU\5coh[SW62aY\pdoFtKGG|c3H5 NYXneI43PzJiaILz M3vEdmFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhmeGG2aYTpd{BEKH[rcoXzJIdmdm:2eYDlJFFjKGmwZnXjeIVlKGmwIFj1TFch[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIILldIxq[2:wIGLORUBt\X[nbDDh[pRmeiB5MjDodpMh[nliVHHxUYFvNWKjc3XkJHJVNVCFUjDhcoFtgXOrczDpckBxemW|ZX7j[UBw\iBzMDWgSmJUNCCHQ{WwQVAvODBzNd88UU4> M3nY[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwPFE5Lz5{NEmwNFgyQDxxYU6=
HuH7 M{\oOGFvfGm4aYLhcEBie3OjeR?= M2fJflczKGi{cx?= NWXvO4N7SW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEOYIHflco91gXCnIELiJIlv\mWldHXkJIlvKGi3bXHuJGh2UDdiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB3cXKjbDDy[ZBtcWOjdHnvckBi\nSncjC3NkBpenNiYomgVnQuWEOUIH3leIhw\CxiRVO1NF0xNjByNd88UU4> M1zMVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OEG5Olc3Lz5{NkixPVY4PjxxYU6=
HuH7 MojNRY51cX[rcnHsJIF{e2G7 NUPzOY9JPzJiaILz MX3BcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDIR3Yh\2Wwb4T5dIUhOmFiaX7m[YN1\WRiaX6gbJVu[W5iSIXIO{Bk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hfmm{YXygVm5CKGyndnXsJIFnfGW{IEeyJIhzeyCkeTDSWE1RS1JibXX0bI9lNCCHQ{WwQVAvODB3NN88UU4> Mo\CQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3OVkoRjJ5OUm0O|U6RC:jPh?=
HuH7 M4\TbmFvfGm4aYLhcEBie3OjeR?= NGHsVWEzPCCqcoO= MWHBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDI[ZBifGm2aYOgR{B3cXK3czDn[Y5wfHmyZTCxZUBqdm[nY4Tl[EBqdiCqdX3hckBJfUh5IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yhfmm{YXygdoVxdGmlYYTpc44h[W[2ZYKgNlQhcHK|IIDy[ZNmdmOnIH;mJFQxLSCQSGOsJGlEPTB;MD6wNFfPxE1w NXGxNWNLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA1PzNpPkK0PVAxPDd|PD;hQi=>
HuH7 NFPudVhCdnSrdnnyZYwh[XO|YYm= Mo\4O|IhcHK| NVXXfmp{SW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEOYIHflco91gXCnIEPhJIlv\mWldHXkJIlvKGi3bXHuJGh2UDdiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB3cXKjbDDy[ZBtcWOjdHnvckBi\nSncjC3NkBpenNiYomgVnQuWEOUIH3leIhw\CxiRVO1NF0xNjByN{NOwG0v M12zVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OEG5Olc3Lz5{NkixPVY4PjxxYU6=
HuH7 M1rydWFvfGm4aYLhcEBie3OjeR?= M1;zNVczKGi{cx?= MXvBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDIR3Yh\2Wwb4T5dIUhO2FiaX7m[YN1\WRiaX6gbJVu[W5iSIXIO{Bk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hfmm{YXygVm5CKGyndnXsJIFnfGW{IEeyJIhzeyCkeTDSWE1RS1JibXX0bI9lNCCHQ{WwQVAvODB5Mt88UU4> MojHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7OUS3OVkoRjJ5OUm0O|U6RC:jPh?=
HuH7 NVHKfWhESW62aY\pdoFtKGG|c3H5 NULqVZJiOjRiaILz M2HBe2FvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhmeGG2aYTpd{BEKH[rcoXzJEhqe2:uYYTlJGNwdjFrIHflco91gXCnIEHiJIlv\mWldHXkJIlvKGi3bXHuJGh2UDdiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB3cXKjbDDy[ZBtcWOjdHnvckBi\nSncjCyOEBpenNiaX6gdJJme2WwY3Wgc4YhPTBnIF7IV{whUUN3ME2wMlAxPzUQvF2u MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyMES3N{c,OjR7MEC0O|M9N2F-
HuH7 M1v5R2FvfGm4aYLhcEBie3OjeR?= NUm4T|Z4PzJiaILz MXLBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDI[ZBifGm2aYOgR{B3cXK3czDn[Y5wfHmyZTCzZUBqdm[nY4Tl[EBqdiCKdVi3JINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiC{ZYDsbYNwdiCUTlGgcIV3\WxiYX\0[ZIhPzJiaILzJIJ6KFSjcV3hck1j[XOnZDDSWE1RS1JiYX7hcJl{cXNiaX6gdJJme2WwY3Wgc4YhOTBnIF\CV{whTUN3ME2wMlAyO87:TT6= MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyMEixPEc,OjR7MEC4NVg9N2F-
HBI10A NVXGN49ISW62aY\pdoFtKGG|c3H5 Ml3kRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTIVx[XSrdHnzJGMhfmm{dYOgd5VjfHmyZTCxZkBqdm[nY4Tl[EBqdiCKQlmxNGEh[2WubIOgbIFz[m:{aX7nJGhEXiC|dXLn[Y5wdWmlIHLpZ4l{fHKxbnnjJJJmeGyrY3;uJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjD2bZJidCC{ZYDsbYNifGmxbjygSWM2OD1yLkCwNu69VS5? Ml7lQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlA3OzB7MD:nQmNpTU2ETEyvZV4>
In vivo In both rat and dog, MK-5172 demonstrates good plasma and liver exposures, with 24-h liver levels suggestive of once-daily dosing. When administered to HCV-infected chimpanzees harboring chronic gt1a or gt1b infections, MK-5172 suppresses viral load between 4 to 5 logs at a dose of 1 mg/kg of body weight twice daily (b.i.d.) for 7 days. MK-5172 demonstrates low to moderate clearance and a modest half-life in both rat and dog. Upon oral administration, MK-5172 demonstrates modest bioavailability of 12 to 13%, with moderate plasma exposure in both species. Significant liver concentrations are achieved in both rat and dog. The 24-h trough liver concentrations are 0.2 μM in rat and 1.4 μM in dog (1 mg per kg), yielding exposure multiples of 27- to 200-fold over the serum-adjusted replicon EC50. MK-5172 proves highly efficacious in vivo at moderate doses against chronic-HCV-infected chimpanzees, including greater viral load suppression than vaniprevir when dosed alternatively to the same animal at an otherwise identical dose and frequency[1].

Protocol (from reference)

Cell Research:[1]
  • Cell lines: HB1 cells
  • Concentrations: 2, 5, or 10 nM
  • Incubation Time: 1, 2, 3.5 days
  • Method: 30,000 HB1 cells are seeded per well of a 6-well tissue culture plate per drug concentration. The next day (day 0), the medium is replenished with fresh medium and MK-5172 at the appropriate drug concentration. Cells from a single well per drug concentration are harvested on days 0, 1, and 2, washed, and stored frozen until evaluation. The fourth well is similarly harvested on day 3.5 except that 30,000 cells are reseeded with fresh medium and MK-5172 at the appropriate drug concentration. For additional time points, cells are passaged and harvested every one-half week for 2 weeks. For the third week, cells are similarly treated except that cells received replenishing medium which contained 0.5 mg/ml G418 without protease inhibitor.
Animal Research:[1]
  • Animal Models: rats or dogs
  • Dosages: 2 mg/kg of body weight (rat) or 0.5 mg/kg (dog)
  • Administration: i.v.

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(130.39 mM)
Water Insoluble
Ethanol '100 mg/mL

Chemical Information

Molecular Weight 766.9
Formula

C38H50N6O9S

CAS No. 1350514-68-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)(C)C1C(=O)N2CC(CC2C(=O)NC3(CC3C=C)C(=O)NS(=O)(=O)C4CC4)OC5=NC6=C(C=CC(=C6)OC)N=C5CCCCCC7CC7OC(=O)N1

In vivo Formulation Calculator (Clear solution)

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

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%DMSO %

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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.
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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03105349 Withdrawn Drug: elbasvir/grazoprevir|Drug: Sofosbuvir|Drug: Ribavirin HCV Fundacion SEIMC-GESIDA July 1 2017 Phase 4
NCT03145623 Completed Drug: Elbasvir and Grazoprevir Hepatitis C|Chronic Kidney Diseases University Hospital Toulouse|MSD France June 2 2017 --
NCT02973503 Completed Drug: Elbasvir/Grazoprevir Fixed Dose Combination Chronic HCV Infection University Hospital Clermont-Ferrand|Merck Sharp & Dohme Corp. January 11 2017 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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