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Chemical Structure| 1350514-68-9 Chemical Structure| 1350514-68-9

Structure of Grazoprevir
CAS No.: 1350514-68-9

Chemical Structure| 1350514-68-9

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Grazoprevir (MK-5172) is a selective hepatitis C virus NS3/4a protease inhibitor with Ki values of 0.01 nM, 0.01 nM, 0.08 nM, 0.15 nM, and 0.90 nM against gt1b, gt1a, gt2a, gt2b, and gt3a, respectively. Grazoprevir inhibits SARS-CoV-2 3CLpro activity.

Synonyms: MK-5172

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Product Details of Grazoprevir

CAS No. :1350514-68-9
Formula : C38H50N6O9S
M.W : 766.90
SMILES Code : O=C([C@H]1N(C([C@@H](N2)C(C)(C)C)=O)C[C@@](OC3=NC4=CC(OC)=CC=C4N=C3CCCCC[C@H]5[C@@H](C5)OC2=O)([H])C1)N[C@]6([C@H](C=C)C6)C(NS(=O)(C7CC7)=O)=O
Synonyms :
MK-5172
MDL No. :MFCD22741510
InChI Key :OBMNJSNZOWALQB-NCQNOWPTSA-N
Pubchem ID :44603531

Safety of Grazoprevir

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • HCV Protease

    gt1a, Ki:0.01 nM

    gt2a, Ki:0.01 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
HB1 cells 6 nM or 30 nM 3 weeks Evaluate the antiviral activity of MK-5172 against genotype 1b replicons, showing that MK-5172 effectively inhibits viral replication even at low concentrations PMC3421554

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Diabetic mouse model Oral administration 3 mg/kg 3 times daily for 10 weeks To evaluate the therapeutic efficacy of the grazoprevir-inducible gene switch in diabetic mice, results showed that oral grazoprevir effectively restored glucose homeostasis. PMC10770082
Chimpanzees Chronic HCV infection model Oral 1 mg/kg Twice daily for 7 days Evaluate the antiviral efficacy of MK-5172 in chronically HCV-infected chimpanzees, showing significant reduction in viral load PMC3421554

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01537900 Hepatitis C PHASE1 COMPLETED 2014-07-31 -
NCT01667081 Hepatitis C COMPLETED 2021-03-31 -
NCT01390428 Hepatitis C PHASE1 COMPLETED 2014-09-12 -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.30mL

0.26mL

0.13mL

6.52mL

1.30mL

0.65mL

13.04mL

2.61mL

1.30mL

References

 

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